The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28248104 |
385 |
Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
Friedrich-Alexander University Erlangen-N£Rnberg |
28214075 |
30 |
Asymmetric total synthesis of tetrahydroprotoberberine derivatives and evaluation of their binding affinities at dopamine receptors. |
Harvard Medical School |
2527994 |
16 |
Conformational analysis and molecular modeling of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as D1 dopamine receptor ligands. |
University of North Carolina |
27688181 |
40 |
Synthesis and evaluation of C9 alkoxy analogues of (-)-stepholidine as dopamine receptor ligands. |
City University of New York |
27876250 |
60 |
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
Jagiellonian University Medical College |
27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
27564135 |
499 |
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists. |
Aptuit |
27132867 |
154 |
Structure-guided development of dualß2 adrenergic/dopamine D2 receptor agonists. |
Friedrich-Alexander University |
27080176 |
117 |
Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists. |
Vanderbilt University |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
27032890 |
52 |
Tetrahydroprotoberberine alkaloids with dopamine ands receptor affinity. |
City University of New York |
26786693 |
153 |
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists. |
Aptuit |
26475518 |
19 |
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor. |
City University of New York |
26288260 |
34 |
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library. |
Universit Degli Studi Di Milano |
26299826 |
112 |
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation. |
Friedrich-Alexander University |
26227779 |
37 |
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold. |
Fudan University |
25076379 |
87 |
Structural manipulation on the catecholic fragment of dopamine D(1) receptor agonist 1-phenyl-N-methyl-benzazepines. |
Shanghai Institute of Materia Medica (Simm) |
25564378 |
56 |
Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
25695425 |
62 |
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
City University of New York |
25734236 |
83 |
Molecular determinants of biased agonism at the dopamine D2 receptor. |
Friedrich-Alexander University |
25969169 |
54 |
A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors. |
University of Barcelona |
25599836 |
14 |
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity. |
Boehringer Ingelheim (Canada) |
25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
25070422 |
126 |
Further evaluation of the tropane analogs of haloperidol. |
Florida A&M University |
25308766 |
56 |
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles. |
Chinese Academy of Sciences |
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 |
25221667 |
66 |
Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity. |
Vanderbilt University |
24831693 |
116 |
Functionally selective dopamine D2, D3 receptor partial agonists. |
Friedrich-Alexander University |
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 |
24900831 |
62 |
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
State Key Laboratory of Drug Research |
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 |
23333208 |
24 |
Design and synthesis of D1 agonist/D2 antagonist for treatment of schizophrenia. |
Sanofi Us |
23332346 |
69 |
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile. |
Chinese Academy of Sciences |
24900647 |
8 |
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand. |
Goethe University |
19796944 |
38 |
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
Universidad De Santiago De Compostela |
18534847 |
37 |
Dopamine/serotonin receptor ligands. Part 17: a cross-target SAR approach: affinities of azecine-styled ligands for 5-HT(2A) versus D1 and D2 receptors. |
Friedrich-Schiller-Universit£T Jena |
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 |
21413808 |
170 |
Synopsis of some recent tactical application of bioisosteres in drug design. |
Bristol-Myers Squibb Pharmaceutical Research and Development |
21381769 |
56 |
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
Universite£ |
23134120 |
72 |
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist. |
University of Innsbruck |
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 |
23018094 |
16 |
Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D3 receptor-selective full agonist ligand. |
Purdue University |
22846798 |
48 |
Chemoenzymatic synthesis and evaluation of 3-azabicyclo[3.2.0]heptane derivatives as dopaminergic ligands. |
University of Tartu |
22748706 |
52 |
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor. |
Shenyang Pharmaceutical University |
22608762 |
25 |
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors. |
Shanghai Institute of Pharmaceutical Industry |
22542010 |
31 |
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition. |
Amgen |
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 |
22537450 |
54 |
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors. |
Gedeon Richter |
21726069 |
98 |
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
University of Namur |
21666830 |
82 |
Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors. |
Harvard Medical School |
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 |
20875743 |
90 |
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela |
Pfizer |
20931963 |
112 |
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. |
Aska Pharmaceutical |
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 |
20041669 |
85 |
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist. |
Chinese Academy of Sciences |
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 |
19744859 |
90 |
Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities? |
Friedrich-Schiller-Universit£T Jena |
19559623 |
33 |
'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity. |
Chinese Academy of Sciences |
19091563 |
79 |
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
Johann Wolfgang Goethe Universit£T |
19331412 |
122 |
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists. |
National Institute On Drug Abuse-Intramural Research Program |
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 |
18361484 |
61 |
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists. |
Egis Pharmaceuticals |
18313303 |
10 |
A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol. |
University Centre For Pharmacy |
17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
18176998 |
45 |
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. |
Abbott Laboratories |
17154515 |
40 |
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
Purdue University |
16480278 |
279 |
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
Organix |
16451077 |
86 |
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists. |
Pfizer |
16420061 |
161 |
Dopamine/serotonin receptor ligands. 10: SAR Studies on azecine-type dopamine receptor ligands by functional screening at human cloned D1, D2L, and D5 receptors with a microplate reader based calcium assay lead to a novel potent D1/D5 selective antagonist. |
University of Bonn |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
16134944 |
85 |
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
Friedrich-Alexander University |
15357957 |
29 |
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers. |
Brigham & Women'S Hospital |
14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
12361386 |
113 |
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. |
Friedrich-Alexander University |
11170639 |
73 |
Current and novel approaches to the drug treatment of schizophrenia. |
Merck Sharp and Dohme Research Laboratories |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
9784114 |
32 |
CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors. |
University of Texas At Austin |
8632409 |
15 |
Comparative molecular field analysis-based prediction of drug affinities at recombinant D1A dopamine receptors. |
Va Medical Center |
7658429 |
31 |
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431). |
Abbott Laboratories |
1531365 |
7 |
A study on the contribution of the 1-phenyl substituent to the molecular electrostatic potentials of some benzazepines in relation to selective dopamine D-1 receptor activity. |
University of Lund |
1531075 |
13 |
(+/-)-3-allyl-7-halo-8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines as selective high affinity D1 dopamine receptor antagonists: synthesis and structure-activity relationship. |
Northeastern University |
1684995 |
27 |
(+/-)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepin, a new high-affinity D1 dopamine receptor ligand: synthesis and structure-activity relationship. |
Northeastern University |
1956042 |
39 |
Fluorescent probes for dopamine receptors: synthesis and characterization of fluorescein and 7-nitrobenz-2-oxa-1,3-diazol-4-yl conjugates of D-1 and D-2 receptor ligands. |
Research Biochemicals |
1973733 |
17 |
Conformational analysis and structure-activity relationships of selective dopamine D-1 receptor agonists and antagonists of the benzazepine series. |
Royal Danish School of Pharmacy |
1977907 |
33 |
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist. |
Abbott Laboratories |
3263503 |
3 |
A photoaffinity label for the D-1 dopamine receptor, (RS)-7-[125I]Iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5- tetrahydro-1H-3-benzazepine, selectively identifies the ligand binding subunits of the receptor. |
Northeastern University |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
22284818 |
4 |
First enantioselective syntheses of the dopamine D1 and D2 receptor modulators, (+)- and (-)-govadine. |
University of British Columbia |
21888437 |
20 |
Chiral indolo[3,2-f][3]benzazecine-type dopamine receptor antagonists: synthesis and activity of racemic and enantiopure derivatives. |
Martin-Luther-Universit£T Halle-Wittenberg |
22204903 |
6 |
Analogues of doxanthrine reveal differences between the dopamine D1 receptor binding properties of chromanoisoquinolines and hexahydrobenzo[a]phenanthridines. |
Quimique C£A. |
21899931 |
27 |
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands. |
The University of Mississippi |
21862338 |
6 |
Assessment of dopamine D¿? receptor affinity and efficacy of three tetracyclic conformationally-restricted analogs of SKF38393. |
Purdue University |
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 |
21550699 |
24 |
New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists. |
University of Tartu |
21555222 |
25 |
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (s) receptor ligands modulates off-target activity and subtype selectivity. |
The University of Sydney |
21334902 |
46 |
Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands. |
Chinese Academy of Sciences |
20949929 |
63 |
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20709559 |
16 |
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists. |
Purdue University |
20620058 |
41 |
Smoothened antagonists for hair inhibition. |
Pfizer |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
20384344 |
42 |
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice. |
Meiji Seika Kaisha |
20180564 |
24 |
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists. |
Friedrich-Schiller-Universit£T Jena |
20064718 |
88 |
Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists. |
Merck Research Laboratories |
20061148 |
73 |
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists. |
Merck Research Laboratories |
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 |
19643610 |
24 |
Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists. |
Schering-Plough Research Institute |
19783143 |
65 |
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead. |
Novartis Institutes For Biomedical Research |
19454369 |
32 |
N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists. |
University of Tartu |
8496700 |
16 |
The Role of Receptor Binding in Drug Discovery |
TBA |
| 21 |
Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamides |
TBA |
| 32 |
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053) |
TBA |
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 |
18835172 |
19 |
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities. |
Chinese Academy of Sciences |
18783955 |
35 |
N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands. |
Chinese Academy of Sciences |
18774793 |
85 |
Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol. |
National Institute On Drug Abuses |
18701276 |
97 |
Highly functionalized 7-azaindoles as selective PPAR gamma modulators. |
Merck Research Laboratories |
18595716 |
142 |
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
Florida A&M University |
18562201 |
13 |
Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. |
Chinese Academy of Sciences |
18053713 |
78 |
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. |
Korea Research Institute of Chemical Technology |
17976986 |
80 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
Pfizer |
17676831 |
67 |
Dopamine/serotonin receptor ligands. 16.(1) Expanding dibenz[d,g]azecines to 11- and 12-membered homologues. Interaction with dopamine D(1)-D(5) receptors. |
Friedrich-Schiller-UniversitäT Jena |
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 |
17539620 |
13 |
Novel ergopeptides as dual ligands for adenosine and dopamine receptors. |
Institut D'Investigacions BiomèDiques August Pi I |
17188870 |
36 |
Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists. |
Friedrich-Schiller-UniversitäT Jena |
17034146 |
24 |
Dopamine/serotonin receptor ligands. 13: Homologization of a benzindoloazecine-type dopamine receptor antagonist modulates the affinities for dopamine D(1)-D(5) receptors. |
Friedrich-Schiller-UniversitäT Jena |
16809034 |
142 |
Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists. |
Schering-Plough Research Institute |
16806922 |
126 |
Modification of the clozapine structure by parallel synthesis. |
Schering-Plough Research Institute |
16759104 |
46 |
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. |
Friedrich-Alexander University |
16722655 |
28 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
Pfizer |
16539400 |
97 |
Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist. |
Friedrich-Schiller-UniversitäT Jena |
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 |
16271293 |
35 |
Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com. |
Abbott |
16216506 |
31 |
3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands. |
Università |
16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College of Physicians and Surgeons |
16134937 |
154 |
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. |
7Tm Pharma |
15771415 |
155 |
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
Johnson & Johnson Pharmaceutical Research & Development |
15293986 |
65 |
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity. |
Friedrich-Schiller-UniversitäT Jena |
15149647 |
10 |
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist. |
Pfizer |
14611858 |
65 |
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands. |
Neurogen |
32107165 |
57 |
Identification of C10 nitrogen-containing aporphines with dopamine D |
City University of New York |
32631561 |
110 |
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
City University of New York |
32631525 |
36 |
Synthesis and dopamine receptor pharmacological evaluations on ring C ortho halogenated 1-phenylbenzazepines. |
City University of New York |
32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
31098001 |
35 |
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
University of Texas Medical Branch |
32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
32282200 |
320 |
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
Shanghaitech University |
10464021 |
59 |
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
Knoll Pharmaceuticals |
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 |
10360732 |
45 |
trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists. |
Abbott Laboratories |
30525590 |
20 |
Novel Strategies To Activate the Dopamine D |
Ucb Pharma |
29939744 |
179 |
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
Shanghaitech University |
9873609 |
15 |
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists. |
Neurogen |
31357129 |
61 |
Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs. |
Medical University of Lublin |
31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
31387791 |
60 |
Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D |
Temple University |
32184974 |
222 |
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands. |
Duke University |
30981605 |
40 |
Chemical synthesis, microbial transformation and biological evaluation of tetrahydroprotoberberines as dopamine D1/D2 receptor ligands. |
Huzhou University |
31938453 |
10 |
Novel Pyrazolyl-dihydroisoquinolines as Positive Allosteric Modulator of the Dopamine D1 Receptor. |
Arrival Discovery |
31532644 |
8 |
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1 |
Amri |
31613617 |
195 |
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
8709107 |
99 |
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
Yamanouchi Pharmaceutical |
26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
7909336 |
27 |
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
R. W. Johnson Pharmaceutical Research Institute |
7830274 |
22 |
Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine receptor ligands. |
Purdue University |
21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
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 |
30383372 |
190 |
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
Huazhong University of Science and Technology |
30344905 |
40 |
New Dopamine D3-Selective Receptor Ligands Containing a 6-Methoxy-1,2,3,4-tetrahydroisoquinolin-7-ol Motif. |
City University of New York |
30431269 |
41 |
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. |
Pfizer |
30389290 |
146 |
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity. |
Texas Tech University Health Sciences Center |
29631959 |
86 |
Synthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine D |
Southern Illinois University Edwardsville |
29767967 |
74 |
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y |
National Institute of Diabetes and Digestive and Kidney Diseases |
28943244 |
136 |
New 5-HT |
Dipartimento Di Farmacia Universit£ |
29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
2405157 |
8 |
Development of a high affinity and stereoselective photoaffinity label for the D-1 dopamine receptor: synthesis and resolution of 7-[125I]iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5-tetrahydro- 1H-3-benzazepine. |
Research Biochemicals |
29965759 |
26 |
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus. |
Janssen Infectious Diseases-Diagnostics |
29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
28495386 |
43 |
Development of molecular tools based on the dopamine D |
Friedrich-Alexander University |
28870802 |
175 |
?-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. |
Friedrich-Alexander University Erlangen-N£Rnberg |
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 |
1652023 |
179 |
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor. |
Abbott Laboratories |
28489379 |
165 |
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for?-Arrestin-Biased D |
Friedrich-Alexander University Erlangen-Nuernberg |
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 |
26851737 |
36 |
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies. |
University of Karachi |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
15850984 |
18 |
Chemistry and biology of dihydroisoxazole derivatives: selective inhibitors of human transglutaminase 2. |
Stanford University |
21113169 |
6 |
Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. |
Cgi Pharmaceuticals |
16509574 |
42 |
Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase. |
Roche Palo Alto |
17010607 |
26 |
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors. |
Abbott Laboratories |
11459666 |
20 |
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. |
Dupont Pharmaceuticals |