The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28089699 |
63 |
Investigation of piperazine benzamides as humanß |
Merck |
28523097 |
37 |
Similarity- and Substructure-Based Development ofß |
Philipps University Marburg |
2859372 |
7 |
Conjugates of catecholamines. 5. Synthesis and beta-adrenergic activity of N-(aminoalkyl)norepinephrine derivatives. |
TBA |
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 |
27692547 |
7 |
Synthesis and activity of newly designed aroxyalkyl or aroxyethoxyethyl derivatives of piperazine on the cardiovascular and the central nervous systems. |
Jagiellonian University Medical College |
27132867 |
154 |
Structure-guided development of dualß2 adrenergic/dopamine D2 receptor agonists. |
Friedrich-Alexander 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 |
26709102 |
142 |
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. |
Merck Research Laboratories |
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 |
25065493 |
92 |
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-actingß2-adrenoceptor agonist. |
Novartis Institutes For Biomedical Research |
24835980 |
98 |
Discovery of TD-4306, a long-actingß2-agonist for the treatment of asthma and COPD. |
Theravance |
24813741 |
110 |
Multivalent design of long-actingß(2)-adrenoceptor agonists incorporating biarylamines. |
Theravance |
16640337 |
47 |
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists. |
Glaxosmithkline |
24100078 |
59 |
Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers. |
Friedrich-Alexander University |
23614528 |
121 |
Synthesis and in vitro and in vivo characterization of highlyß1-selectiveß-adrenoceptor partial agonists. |
University of Nottingham |
23614494 |
2 |
Structure-based fragment screening is demonstrated to be a practical lead discovery method for a representative G-protein-coupled receptor. |
Pfizer |
23517028 |
2 |
Biophysical fragment screening of theß1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design. |
Heptares Therapeutics |
21870877 |
119 |
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for humanß-adrenoceptors. |
University of Nottingham |
17507221 |
58 |
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
Novartis Institutes For Biomedical Research |
16759089 |
5 |
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. |
The University of Melbourne |
11806709 |
63 |
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres. |
Glaxosmithkline |
1346651 |
29 |
Synthesis of halogenated trimetoquinol derivatives and evaluation of their beta-agonist and thromboxane A2 (TXA2) antagonist activities. |
Ohio State University |
22932315 |
28 |
An investigation into the structure-activity relationships associated with the systematic modification of theß(2)-adrenoceptor agonist indacaterol. |
Novartis Institutes For Biomedical Research |
22079756 |
219 |
From libraries to candidate: the discovery of new ultra long-acting dibasicß2-adrenoceptor agonists. |
Astrazeneca |
22178551 |
46 |
A multivalent approach to the discovery of long-actingß(2)-adrenoceptor agonists for the treatment of asthma and COPD. |
Theravance |
21925889 |
48 |
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating a urea group. |
Glaxosmithkline |
21696967 |
51 |
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating hydantoin or uracil rings. |
Glaxosmithkline |
21723724 |
91 |
Design-driven LO: the discovery of new ultra long acting dibasicß2-adrenoceptor agonists. |
Astrazeneca |
20462258 |
50 |
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach. |
Glaxosmithkline |
19317397 |
62 |
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups. |
Glaxosmithkline |
9548813 |
53 |
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. |
Smithkline Beecham Pharmaceuticals |
6330358 |
6 |
The 3,4-catechol derivative of propranolol, a minor dihydroxylated metabolite. |
TBA |
6148422 |
36 |
Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers. |
TBA |
6134834 |
54 |
Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class. |
TBA |
6130154 |
68 |
Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function. |
TBA |
6130153 |
66 |
Ultra-short-acting beta-adrenergic receptor blocking agents. 1. (Aryloxy)propanolamines containing esters in the nitrogen substituent. |
TBA |
6120237 |
15 |
2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents. |
TBA |
6104730 |
47 |
Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers. |
TBA |
11454468 |
35 |
Discovery and SAR of org 24598-a selective glycine uptake inhibitor. |
Organon Research and Development Group |
21486038 |
177 |
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. |
H. Lundbeck |
22386241 |
46 |
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents. |
Sk Biopharmaceuticals |
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 |
24900353 |
6 |
Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity. |
TBA |
24900360 |
24 |
Synthesis and Cardiac Imaging of (18)F-Ligands Selective for ß1-Adrenoreceptors. |
TBA |
21726069 |
98 |
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
University of Namur |
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 |
20181479 |
177 |
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles. |
Merck Research Laboratories |
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 |
19608416 |
29 |
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the beta2-adrenergic receptor: part 6. |
Astellas Pharma |
19581100 |
162 |
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists. |
Astellas Pharma |
19232786 |
72 |
Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists. |
Astellas Pharma |
18651730 |
123 |
Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety. |
Astellas Pharma |
16562853 |
22 |
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro. |
Tom'S of Maine |
18307290 |
97 |
Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I. |
Astellas Pharma |
16451077 |
86 |
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists. |
Pfizer |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
16250647 |
71 |
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
Universit£ |
15603933 |
28 |
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist. |
Fujisawa Pharmaceutical |
12213075 |
70 |
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). |
Purdue University |
11311069 |
64 |
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
Wyeth-Ayerst Research |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
7562902 |
114 |
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. |
Smithkline Beecham Pharmaceuticals |
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 |
8254623 |
54 |
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity. |
National Institute of Diabetes and Digestive and Kidney Diseases |
8230093 |
34 |
Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives. |
Universit£ |
1313109 |
40 |
Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors. |
Universit£ |
1359141 |
47 |
Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines. |
Merck Sharp and Dohme Research Laboratories |
2319556 |
16 |
Synthesis and pharmacological studies of N-[4-[2-hydroxy-3-[[2-[4-(1H-imidazol-1- yl)phenoxy]ethyl]amino]propoxy]phenyl]methanesulfonamide, a novel antiarrhythmic agent with class II and class III activities. |
Berlex Laboratories |
1976812 |
62 |
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
Berlex Laboratories |
2845082 |
35 |
Syntheses and adrenergic activities of ring-fluorinated epinephrines. |
National Institute of Diabetes |
6126588 |
12 |
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene. |
TBA |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
| 8 |
Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibition |
TBA |
21863888 |
9 |
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease. |
Pfizer |
21783363 |
10 |
Synthesis and in vitro evaluation of derivatives of theß¿?-adrenergic receptor antagonist HX-CH 44. |
University of Toronto |
20036561 |
39 |
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists. |
Medical University of Lublin |
21353541 |
25 |
Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective humanß3 adrenergic receptor agonists. |
Merck Research Laboratories |
21277205 |
26 |
Discovery of substituted phenyl urea derivatives as novel long-actingß2-adrenoreceptor agonists. |
RhôNe-Poulenc Rorer |
20833036 |
221 |
Thienopyrimidines asß3-adrenoceptor agonists: hit-to-lead optimization. |
4Sc |
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 |
20655218 |
72 |
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators. |
Novartis Institutes For Biomedical Research |
20684592 |
83 |
Identification of potent and selective amidobipyridyl inhibitors of protein kinase D. |
Novartis Institutes For Biomedical Research |
20684591 |
87 |
Identification of orally available naphthyridine protein kinase D inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
20434333 |
111 |
A vHTS approach for the identification of beta-adrenoceptor ligands. |
4Sc |
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 |
20096576 |
41 |
Discovery of olodaterol, a novel inhaled beta2-adrenoceptor agonist with a 24 h bronchodilatory efficacy. |
Boehringer Ingelheim Pharma |
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 |
19643607 |
26 |
Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action. |
Boehringer Ingelheim Pharma |
19875286 |
44 |
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as beta2-adrenoceptor agonists. |
Boehringer Ingelheim Pharma |
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 |
| 38 |
Carboxyl-promoted enhancement of selectivity for the β3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β3 binding selectivity |
TBA |
| 7 |
SYNTHESIS AND BIOLOGICAL EVALUATION OF A FLUORINATED ANALOG OF THE β-ADRENERGIC BLOCKING AGENT, METOPROLOL |
TBA |
| 26 |
BMS-187257, a potent, selective, and novel heterocyclic β3 adrenergic receptor agonist |
TBA |
| 3 |
Asymmetric synthesis of FR165914: A novel β3-adrenergic agonist with a benzocycloheptene structure |
TBA |
19492813 |
56 |
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues. |
Glaxosmithkline |
19366244 |
138 |
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5. |
Astellas Pharma |
19362005 |
74 |
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists. |
Astellas Pharma |
19131251 |
9 |
Preliminary evaluation of pharmacological properties of some xanthone derivatives. |
Jagiellonian University Medical College |
19081260 |
10 |
Substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes as beta3-adrenergic receptor agonists: design, synthesis, biological evaluation and pharmacophore modeling. |
Central Drug Research Institute |
18752946 |
47 |
Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV. |
Astellas Pharma |
18701276 |
97 |
Highly functionalized 7-azaindoles as selective PPAR gamma modulators. |
Merck Research Laboratories |
18656910 |
2 |
Facile radiosynthesis of fluorine-18 labeled beta-blockers. Synthesis, radiolabeling, and ex vivo biodistribution of [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol. |
Centre For Addiction and Mental Health |
18640038 |
74 |
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. |
Amgen |
18599160 |
4 |
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1. |
RzeszóW University of Technology |
18553954 |
126 |
Discovery of a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II. |
Astellas Pharma |
17911024 |
37 |
Potent oxindole based human beta3 adrenergic receptor agonists. |
Eli Lilly |
17804228 |
44 |
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. |
Eli Lilly |
17632003 |
55 |
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity. |
Pfizer |
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 |
17533126 |
78 |
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17524641 |
69 |
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists. |
Glaxosmithkline |
17506540 |
52 |
Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor. |
Medical University of Lublin |
17303428 |
22 |
Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes. |
Università |
16931005 |
21 |
Potent benzimidazolone based human beta(3)-adrenergic receptor agonists. |
Eli Lilly |
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 |
16361098 |
70 |
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists. |
F. Hoffmann-La Roche |
15686912 |
35 |
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety. |
Dainippon Pharmaceutical |
15546708 |
35 |
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives. |
Dainippon Pharmaceutical |
15546707 |
60 |
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring. |
Dainippon Pharmaceutical |
14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
12798332 |
35 |
Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists. |
Wyeth Research |
12657269 |
52 |
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines. |
Dainippon Pharmaceutical |
12361399 |
17 |
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. |
Universita Di Camerino |
12270184 |
34 |
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines. |
Wyeth Research |
12270183 |
45 |
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines. |
Wyeth Research |
11720857 |
37 |
4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor. |
Wyeth-Ayerst Research |
11327605 |
27 |
New oxadiazolidinedione derivatives as potent and selective human beta3 agonists. |
Wyeth-Ayerst Research |
11277513 |
25 |
2,4-Thiazolidinediones as potent and selective human beta3 agonists. |
Wyeth-Ayerst Research |
11212115 |
72 |
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties. |
Merck Research Laboratories |
32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
31753798 |
49 |
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent ? |
Shenyang Pharmaceutical University |
11055339 |
59 |
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists. |
Merck Research Laboratories |
11052788 |
33 |
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide. |
Merck Research Laboratories |
10999482 |
52 |
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides. |
Merck Research Laboratories |
10987429 |
69 |
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore. |
Merck Research Laboratories |
10915043 |
69 |
Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists. |
Merck Research Laboratories |
10888325 |
90 |
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents. |
Merck Research Laboratories |
10888324 |
48 |
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist. |
Merck Research Laboratories |
10780918 |
27 |
Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities. |
National Institute of Diabetes and Digestive and Kidney Diseases |
10743949 |
76 |
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents. |
Università |
31625751 |
12 |
Synthesis, Purification, and Selective ? |
Shandong University |
32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
31151791 |
35 |
Development of covalent antagonists for ?1- and ?2-adrenergic receptors. |
Friedrich-Alexander Universit£T Erlangen-N£Rnberg |
31042379 |
96 |
Hybridization of ?-Adrenergic Agonists and Antagonists Confers G Protein Bias. |
Friedrich-Alexander University Erlangen-N£Rnberg (Fau) |
10406657 |
91 |
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore. |
Merck Research Laboratories |
30875219 |
254 |
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D |
University of North Carolina At Chapel Hill |
10360736 |
2 |
S1319: a novel beta2-andrenoceptor agonist from a marine sponge Dysidea sp. |
Kirin Brewery |
10340609 |
15 |
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability. |
Merck Research Laboratories |
10201842 |
69 |
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides. |
Merck Research Laboratories |
10201841 |
47 |
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides. |
Merck Research Laboratories |
31298548 |
112 |
Probing the Existence of a Metastable Binding Site at the ? |
University of Copenhagen |
9876110 |
58 |
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
Centro De InvestigacióN Grupo Ferrer |
9873681 |
65 |
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists. |
Merck Research Laboratories |
9873496 |
80 |
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties. |
Merck Research Laboratories |
31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
9871717 |
72 |
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. |
Merck Research Laboratories |
9871716 |
94 |
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor. |
Merck Research Laboratories |
30392952 |
49 |
Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent ? |
Shenyang Pharmaceutical University |
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 |
31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
26590100 |
42 |
Discovery of benzamides as potent human ?3 adrenergic receptor agonists. |
Merck And |
26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
31223445 |
4 |
Computer-Aided Selective Optimization of Side Activities of Talinolol. |
Goethe-University of Frankfurt |
8093626 |
13 |
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents. |
Università |
7910217 |
36 |
The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. |
Universitá |
21170122 |
84 |
Comparative 3D QSAR study on ?(1)-, ?(2)-, and ?(3)-adrenoceptor agonists. |
National Institute of Pharmaceutical Education and Research |
21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
17560786 |
48 |
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids. |
Glaxosmithkline |
17129726 |
121 |
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
10377236 |
15 |
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists. |
University of Tennessee |
8809159 |
26 |
Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands. |
University of Tennessee-Memphis |
29751236 |
46 |
Synthesis and biological evaluation of ? |
Shenyang Pharmaceutical University |
29574204 |
54 |
Design and synthesis of aryloxypropanolamine as ? |
East China Normal University |
2892936 |
21 |
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. |
Warner-Lambert |
2875184 |
57 |
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
TBA |
29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
29425815 |
76 |
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT |
Jagiellonian University Medical College |
2563296 |
38 |
A new series of tricyclic (aryloximino)propanolamines displaying very high selective beta 2-blocking properties. |
Université |
29851481 |
122 |
Discovery of ?-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
University of Florence |
29706529 |
22 |
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone. |
Jagiellonian University Medical College |
29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
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£ |
1672155 |
14 |
Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol. |
National Institute of Diabetes |
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 |
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 |
1347318 |
52 |
Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents. |
Berlex Laboratories |
| 7 |
Synthesis and pharmacological evaluation of 4-[2- hydroxy-3-(4-phenyl-piperazin-1-yl)-propoxy]-4- azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione |
The Medical University of Warsaw |
19337725 |
43 |
Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. |
Case Western Reserve University |
16915381 |
31 |
WAY-100635 is a potent dopamine D4 receptor agonist. |
Purdue University |
16352709 |
44 |
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis. |
Mcgill University |
15831442 |
46 |
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke. |
Taisho Pharmaceutical |
15131245 |
86 |
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization. |
Sanofi-Synthelabo Recherche |
14730417 |
62 |
Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. |
UniversitÄT WÜRzburg |
12784105 |
53 |
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. |
Case Western Reserve University |
12761331 |
97 |
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. |
Case Western Reserve University |
12649361 |
779 |
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists. |
Case Western Reserve University |
12431845 |
84 |
Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder. |
Eli Lilly |
12388666 |
301 |
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
Institut De Recherches Servier |
12192085 |
52 |
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. |
Case Western Reserve University |
12110997 |
380 |
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs. |
WestfÄLische Wilhelms-UniversitÄ |
11750183 |
29 |
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. |
Novartis Pharma |
11750180 |
139 |
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. |
Eli Lilly |
11512051 |
80 |
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. |
Case Western Reserve University |
11438309 |
51 |
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. |
Janssen Research Foundation |
11356907 |
15 |
Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization. |
Institut De Recherches Servier |
11082457 |
63 |
S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. |
Centre De Recherches De Croissy |
11082453 |
77 |
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse. |
Abbott Laboratories |
9454810 |
72 |
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. |
Sanofi Recherche |
9225287 |
174 |
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. |
Roche Bioscience |
9144661 |
24 |
BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats. |
Smithkline Beecham Pharmaceuticals |
8935801 |
586 |
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
Janssen Research Foundation |
8788493 |
64 |
Novel discriminatory ligands for 5-HT2B receptors. |
Smithkline Beecham Pharmaceuticals |
8730737 |
23 |
Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety. |
Smithkline Beecham Pharmaceuticals |
8584042 |
40 |
BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex. |
Boehringer Ingelheim Italia |
8564196 |
35 |
Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo. |
Syntex Discovery Research |
8012715 |
38 |
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. |
Glaxo Group Research |
7921604 |
16 |
The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon. |
Smithkline Beecham Pharmaceuticals |
7915318 |
120 |
Biochemical and pharmacological characterization of high-affinity trimetoquinol analogs on guinea pig and human beta adrenergic receptor subtypes: evidence for partial agonism. |
Ohio State University |
2530094 |
94 |
The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. |
Novo Industri |
1982626 |
30 |
Neurochemical profile of eltoprazine. |
Duphar |
1968985 |
56 |
Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents. |
Niigata College of Pharmacy |
1661335 |
95 |
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins. |
Center For Bio-Pharmaceutical Sciences |
15655528 |
75 |
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. |
University of Nottingham |