The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28375629 |
84 |
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain. |
Pfizer |
| 28319392 |
216 |
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 2879916 |
20 |
Conformationally defined adrenergic agents. 4. 1-(aminomethyl)phthalans: synthesis and pharmacological consequences of the phthalan ring oxygen atom. |
TBA |
| 12749888 |
63 |
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists. |
Roche Bioscience |
| 12392747 |
36 |
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. |
Glaxosmithkline |
| 27689727 |
46 |
Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT |
Universit£ |
| 27866818 |
84 |
The discovery of quinoline based single-ligand human H |
Glaxosmithkline |
| 27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
| 27448917 |
33 |
Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists ofa1-adrenoceptor. |
University of Bras£Lia |
| 27658792 |
24 |
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines asa |
Jagiellonian University Medical College |
| 27709945 |
62 |
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea |
Chinese Academy of Sciences |
| 27031406 |
114 |
Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selectivea1A-Adrenoceptor Antagonists. |
Chengdu University |
| 27173799 |
97 |
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics. |
Shanghai Institute of Materia Medica |
| 26954848 |
38 |
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. |
Takeda Pharmaceutical |
| 26723530 |
68 |
Improving selectivity of dopamine D3 receptor ligands. |
Bioprojet-Biotech |
| 26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
| 26125514 |
40 |
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Humanß3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects. |
Asahi Kasei Pharma |
| 25288493 |
96 |
Human alpha1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines. |
Unsw Australia |
| 25261823 |
107 |
Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands ata<alpha>1 and 5-HT1A receptors. |
Universit£ |
| 26005522 |
32 |
Discovery of Quinazoline-Based Fluorescent Probes toa1-Adrenergic Receptors. |
Shandong University |
| 25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
| 25813897 |
12 |
a-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one. |
Jagiellonian University Medical College |
| 25754490 |
44 |
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker. |
Novartis Pharma |
| 24863744 |
15 |
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
University of Missouri |
| 25241924 |
47 |
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor. |
Novartis Institutes For Biomedical Research |
| 24992070 |
51 |
High affinity ligands and potent antagonists for thea1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives. |
Universit£ |
| 24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
| 24800940 |
146 |
Identification of a new selective dopamine D4 receptor ligand. |
Florida A&M University |
| 24559051 |
141 |
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
Intra-Cellular Therapies |
| 23252794 |
56 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives ina1-adrenergic and 5-HT1A receptor binding sites recognition. |
University of Camerino |
| 12643939 |
81 |
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds. |
Glaxosmithkline |
| 11844675 |
114 |
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series. |
Glaxosmithkline |
| 11814822 |
108 |
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
Glaxosmithkline |
| 12443779 |
44 |
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties. |
Janssen-Cilag |
| 12419381 |
95 |
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
Glaxosmithkline |
| 11597419 |
105 |
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
Glaxosmithkline |
| 22370341 |
29 |
Favourable involvement ofa2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement. |
University of Camerino |
| 22145629 |
68 |
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergica1- and serotonine 5-HT1A receptors. |
Universit£ |
| 21514979 |
92 |
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands fora1-adrenoceptor subtypes. |
Universit£ |
| 20934789 |
27 |
Synthesis anda1-adrenoceptor antagonist activity of tamsulosin analogues. |
Universit£ |
| 20951033 |
59 |
Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists. |
Glaxosmithkline |
| 20801662 |
60 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study. |
Universit£ |
| 20605276 |
61 |
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
Universit£ |
| 20674357 |
66 |
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders. |
Glaxosmithkline |
| 20185311 |
72 |
Discovery of a new series of 5-HT1A receptor agonists. |
Universit£ |
| 19719240 |
25 |
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity. |
University of Camerino |
| 18817363 |
84 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
Universit£ |
| 17125266 |
72 |
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?). |
Universit£ |
| 11755365 |
113 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2. |
Janssen-Cilag |
| 11755364 |
104 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1. |
Janssen-Cilag |
| 11454468 |
35 |
Discovery and SAR of org 24598-a selective glycine uptake inhibitor. |
Organon Research and Development Group |
| 10636247 |
83 |
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants. |
Janssen Research Foundation |
| 22959245 |
175 |
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs). |
The University of Sydney |
| 23009245 |
53 |
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence. |
Sanford-Burnham Medical Research Institute |
| 22650618 |
4 |
Rediocide A, an Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C. |
Chinese Academy of Sciences |
| 22738628 |
38 |
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. |
University of Li£Ge |
| 23124215 |
72 |
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selectivea1B-adrenoceptor antagonist. |
Universit£ |
| 22985961 |
99 |
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
Glaxosmithkline |
| 22313227 |
78 |
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. |
National Institute of Mental Health |
| 21859078 |
62 |
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with highs1 receptor affinity. |
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster |
| 21634396 |
55 |
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
Cephalon |
| 21207959 |
69 |
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging. |
National Institute of Mental Health |
| 20684563 |
176 |
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. |
H. Lundbeck |
| 19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
Hunter College and The Graduate Center of The City University of New York |
| 18468904 |
48 |
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand. |
Purdue University |
| 18400496 |
112 |
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
Pfizer |
| 18361484 |
61 |
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists. |
Egis Pharmaceuticals |
| 17407815 |
27 |
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. |
Janssen-Cilag |
| 16451077 |
86 |
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists. |
Pfizer |
| 16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
| 15482914 |
25 |
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750. |
Pfizer |
| 14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
| 12825930 |
16 |
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes. |
Universit£ |
| 12825922 |
207 |
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
Virginia Commonwealth University |
| 11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
| 10579843 |
81 |
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series. |
Synaptic Pharmaceutical |
| 10579840 |
88 |
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones. |
Synaptic Pharmaceutical |
| 9135028 |
114 |
Pharmacological options in the treatment of benign prostatic hyperplasia. |
Pfizer |
| 7562902 |
114 |
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. |
Smithkline Beecham Pharmaceuticals |
| 7752182 |
41 |
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. |
Synaptic Pharmaceutical |
| 1833546 |
47 |
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands. |
Abbott Laboratories |
| 2845082 |
35 |
Syntheses and adrenergic activities of ring-fluorinated epinephrines. |
National Institute of Diabetes |
| 2982020 |
2 |
N-[2-hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide. A potent agonist which releases intracellular calcium by activation of alpha 1-adrenoceptors. |
TBA |
| 6118438 |
12 |
Alpha-adrenergic agents. 1. Direct-acting alpha 1 agonists related to methoxamine. |
TBA |
| 15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
| 11354357 |
61 |
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien. |
Abbott Laboratories |
| 11078200 |
61 |
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists. |
Welfide |
| 10987417 |
48 |
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists. |
Merck Research Laboratories |
| 10522703 |
103 |
Design and synthesis of novel dihydropyridine alpha-1a antagonists. |
Synaptic Pharmaceutical |
| 9873568 |
22 |
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity. |
Merck |
| 22000209 |
54 |
Design, synthesis and in vitro evaluation of bridgehead fluoromethyl analogs of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) for the 5-HT(1A) receptor. |
Vu University Medical Center |
| 21788137 |
33 |
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands. |
The University of Sydney |
| 21591752 |
41 |
Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile. |
Soochow University College of Pharmaceutical Sciences |
| 21520940 |
40 |
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. |
Vu University Medical Center |
| 20812727 |
157 |
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography. |
National Institute of Mental Health |
| 20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
| 20681583 |
7 |
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities. |
Hokkaido University |
| 20709559 |
16 |
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists. |
Purdue University |
| 20708933 |
60 |
Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands. |
Université |
| 20620058 |
41 |
Smoothened antagonists for hair inhibition. |
Pfizer |
| 19646882 |
72 |
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj |
| 19773162 |
72 |
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. |
Arena Pharmaceuticals |
| | 26 |
Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptor |
TBA |
| | 32 |
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053) |
TBA |
| | 14 |
Marine sponge bis(indole) alkaloids that displace ligand binding to α1 adrenergic receptors |
TBA |
| | 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
TBA |
| | 37 |
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists. |
TBA |
| 19414260 |
85 |
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
Pfizer |
| 19403308 |
36 |
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists. |
Tsukuba Research Institute |
| 19394220 |
71 |
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks. |
Pfizer |
| 19329329 |
183 |
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET. |
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz |
| 18980842 |
21 |
Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists. |
Pfizer |
| 18952421 |
60 |
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 18783208 |
11 |
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function. |
National Institute of Mental Health |
| 18378462 |
5 |
Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents. |
Sinhgad College of Pharmacy |
| 17904840 |
64 |
Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS). |
Johnson & Johnson Pharmaceutical Research and Development |
| 17668922 |
63 |
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits. |
Lundbeck Research Usa |
| 17571866 |
49 |
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. |
National Institute of Mental Health |
| 17524641 |
69 |
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists. |
Glaxosmithkline |
| 17517507 |
131 |
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS). |
Johnson & Johnson Pharmaceutical Research and Development |
| 17452102 |
227 |
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS). |
Johnson & Johnson Pharmaceutical Research and Development |
| 17254786 |
30 |
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands. |
Johnson & Johnson Pharmaceutical Research and Development |
| 16730981 |
22 |
Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility. |
Lundbeck Research Usa |
| 16621538 |
35 |
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol. |
Florida A&M University |
| 16458504 |
37 |
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand. |
Columbia University College of Physicians and Surgeons |
| 16392816 |
113 |
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. |
Alcon Research |
| 16392798 |
46 |
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. |
Columbia University College of Physicians and Surgeons |
| 16153828 |
22 |
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists. |
Chungbuk National University |
| 15828846 |
47 |
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists. |
Lundbeck Research Usa |
| 15771448 |
187 |
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity. |
Janssen-Cilag |
| 15715476 |
4 |
Structure-based drug discovery using GPCR homology modeling: successful virtual screening for antagonists of the alpha1A adrenergic receptor. |
Aventis Pharma Deutschland |
| 15664832 |
45 |
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. |
China Pharmaceutical University |
| 15341484 |
159 |
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors. |
Merck |
| 15341483 |
110 |
Indolebutylamines as selective 5-HT(1A) agonists. |
Merck |
| 15324890 |
29 |
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. |
Virginia Commonwealth University |
| 15149647 |
10 |
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist. |
Pfizer |
| 14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
| 14611858 |
65 |
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands. |
Neurogen |
| 12904082 |
20 |
New potential uroselective NO-donor alpha1-antagonists. |
Università |
| 12617901 |
23 |
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists. |
F. Hoffmann-La Roche |
| 12238918 |
22 |
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine. |
Abbott Laboratories |
| 12161153 |
39 |
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists. |
Johnson & Johnson Pharmaceutical Research and Development |
| 12127524 |
39 |
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia. |
Johnson & Johnson Pharmaceutical Research and Development |
| 11728188 |
53 |
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
Università |
| 11514163 |
14 |
Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist. |
F. Hoffmann-La Roche |
| 32130004 |
4 |
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma. |
Celgene |
| 11459670 |
30 |
Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists. |
Merck |
| 11448222 |
80 |
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
Istituto Chimico Farmaceutico E Tossicologico |
| 32122737 |
85 |
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics. |
University of Chinese Academy of Sciences |
| 32073845 |
74 |
Discovery of 4-((2 S,4 S)-4-Ethoxy-1-((5-methoxy-7-methyl-1 H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases |
Novartis Institutes For Biomedical Research |
| 32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
| 11133073 |
12 |
Determination of the relative and absolute stereochemistry of a potent and alpha1A-selective adrenoceptor antagonist. |
Synaptic Pharmaceutical |
| 11055359 |
18 |
Novel heterocycles as selective alpha1-adrenergic receptor antagonists. |
The R. W. Johnson Pharmaceutical Research Institute |
| 10956183 |
19 |
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability. |
Synaptic Pharmaceutical |
| 10937710 |
81 |
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones. |
Merck |
| 10937709 |
87 |
Phenylacetamides as selective alpha-1A adrenergic receptor antagonists. |
Merck |
| 10893308 |
102 |
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia. |
Merck Research Laboratories |
| 10843225 |
36 |
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. |
The R. W. Johnson Pharmaceutical Research Institute |
| 10841797 |
110 |
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists. |
The R. W. Johnson Pharmaceutical Research Institute |
| 10673105 |
38 |
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists. |
Synaptic Pharmaceutical |
| 31668424 |
17 |
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders. |
Marquette University |
| 10579842 |
91 |
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains. |
Synaptic Pharmaceutical |
| 10579841 |
113 |
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety. |
Synaptic Pharmaceutical |
| 32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
| 10464027 |
118 |
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists. |
University of Oregon |
| 31021617 |
136 |
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D |
University of Pennsylvania |
| 30875219 |
254 |
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D |
University of North Carolina At Chapel Hill |
| 30844609 |
101 |
Chemical manipulations on the 1,4-dioxane ring of 5-HT |
Universit£ |
| 10021947 |
44 |
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists. |
Merck |
| 31834797 |
31 |
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
University of Florida |
| 9986714 |
105 |
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists. |
Recordati |
| 9888842 |
21 |
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton. |
Università |
| 9873563 |
67 |
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists. |
Merck |
| 31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
| 9871673 |
79 |
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates. |
Wyeth-Ayerst Research Laboratories |
| 31743642 |
198 |
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual ?-Opioid Receptor Agonists and ? |
Esteve Pharmaceuticals |
| 9857099 |
94 |
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia. |
Synaptic Pharmaceutical |
| 31112892 |
84 |
1,3-Dioxane as a scaffold for potent and selective 5-HT |
Universit£ |
| 9548811 |
55 |
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist. |
Merck |
| 9379432 |
36 |
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign pr |
Abbott Laboratories |
| 31613617 |
195 |
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
| 30715878 |
68 |
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. |
Genentech |
| 31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
| 26643219 |
69 |
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as ?1A/1D-AR subselective antagonists for BPH. |
Jinan University |
| 26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
| 25281269 |
35 |
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists. |
Astellas Pharma |
| 23902232 |
42 |
6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective ?1D-adrenoceptor antagonist. |
Universit£ |
| 7658428 |
94 |
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. |
Smithkline Beecham Pharmaceuticals |
| 21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
| 17027264 |
33 |
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes. |
Universit£ |
| 16302814 |
55 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtypes in the regulation of human PC-3 prostate |
Universit£ |
| 14584940 |
30 |
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors. |
University of Bologna |
| 12014961 |
287 |
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues. |
Glaxosmithkline Research Laboratories |
| 10514291 |
51 |
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
University of Bologna |
| 10425105 |
51 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
University of Camerino |
| 9651170 |
189 |
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate. |
New York University Medical Center |
| 8917649 |
60 |
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist. |
University of Camerino |
| 8831777 |
48 |
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist. |
Abbott Laboratories |
| 8057272 |
33 |
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists. |
Glaxo Research and Development |
| 29324345 |
122 |
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect. |
Shanghai Institute of Materia Medica |
| 29291438 |
46 |
Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HT |
Shanghai Institute of Pharmaceutical Industry |
| 29615343 |
18 |
Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives. |
Luoyang Normal University |
| 29944371 |
79 |
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain. |
Pfizer |
| 29730027 |
99 |
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system. |
Jagiellonian University Medical College |
| 28800452 |
44 |
Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective ? |
Takeda Pharmaceutical |
| 29767967 |
74 |
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 29422390 |
3 |
Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on ? |
Guangzhou Medical University |
| 29395980 |
84 |
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs. |
University of Chinese Academy of Sciences |
| 29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
| 28499171 |
36 |
Quinazoline based ? |
Alma Mater Studiorum-University of Bologna |
| 29784274 |
40 |
Chiral analogues of (+)-cyclazosin as potent? |
Universit£ |
| 28355078 |
34 |
Discovery of Novel Indazole Derivatives as Orally Available? |
Asahi Kasei Pharma |
| 29589445 |
154 |
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
Universit£ |
| 28774576 |
134 |
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics. |
Xinjiang Technical Institute of Physics and Chemistry |
| 27662034 |
69 |
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT |
Universit£ |
| 28489950 |
119 |
Return of D |
University of Nebraska Medical Center |
| 1674541 |
24 |
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity. |
Harvard Medical School |
| 28342939 |
12 |
Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review. |
Indo-Soviet Friendship College of Pharmacy (Isfcp) |
| 1354264 |
19 |
Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. |
American Cyanamid |
| 27288643 |
16 |
Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives. |
Birla Institute of Technology |
| 27231829 |
34 |
New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives. |
Universidade De Evora |
| 27049670 |
47 |
Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. |
Max Planck Institute of Molecular Physiology |
| 26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
| 26943478 |
16 |
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
Chulabhorn Research Institute |
| 26518975 |
9 |
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues. |
Peking University |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
| 26214585 |
23 |
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents. |
University of Wisconsin-Madison |
| 25459661 |
19 |
Inhibition of AMP deaminase activity does not improve glucose control in rodent models of insulin resistance or diabetes. |
Astrazeneca R&D |
| 25462626 |
6 |
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes. |
Comsats Institute of Information Technology |
| 18201066 |
48 |
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships. |
Nerviano Medical Sciences |
| 19115845 |
39 |
First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. |
Nerviano Medical Sciences |
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