Page last updated: 2024-08-07 15:47:29
Beta-1 adrenergic receptor
A beta-1 adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08588]
Synonyms
Beta-1 adrenoreceptor;
Beta-1 adrenoceptor
Research
Bioassay Publications (98)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 8 (8.16) | 18.7374 |
| 1990's | 13 (13.27) | 18.2507 |
| 2000's | 33 (33.67) | 29.6817 |
| 2010's | 40 (40.82) | 24.3611 |
| 2020's | 4 (4.08) | 2.80 |
Compounds (104)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
[no title available]Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Recent Advances in βJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
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.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
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: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
[no title available],
Volume of Distribution in Drug Design.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
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.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Similarity- and Substructure-Based Development of βACS medicinal chemistry letters, , May-11, Volume: 8, Issue:5, 2017
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as beta2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available]Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
8-Hydroxyquinolin-2(1H)-one analogues as potential βEuropean journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
[no title available]Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Synthesis and biological evaluation of βEuropean journal of medicinal chemistry, , May-25, Volume: 152, 2018
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , May-01, Volume: 17, Issue:9, 2009
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.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
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.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
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.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 2006
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.Journal of medicinal chemistry, , Jan-31, Volume: 45, Issue:3, 2002
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
[no title available],
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Volume of Distribution in Drug Design.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available],
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
[no title available],
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.Journal of medicinal chemistry, , Volume: 27, Issue:8, 1984
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.Journal of medicinal chemistry, , Volume: 26, Issue:2, 1983
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.Journal of medicinal chemistry, , Jan-08, Volume: 36, Issue:1, 1993
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.Journal of medicinal chemistry, , Volume: 27, Issue:8, 1984
Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
[no title available],
8-Hydroxyquinolin-2(1H)-one analogues as potential βEuropean journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Recent Advances in βJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent βBioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
[no title available]Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents.Journal of medicinal chemistry, , Feb-21, Volume: 35, Issue:4, 1992
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
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.Journal of medicinal chemistry, , Volume: 33, Issue:4, 1990
[no title available],
Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents.Journal of medicinal chemistry, , Feb-21, Volume: 35, Issue:4, 1992
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
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 bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
2,4-Thiazolidinediones as potent and selective human beta3 agonists.Bioorganic & medicinal chemistry letters, , Mar-26, Volume: 11, Issue:6, 2001
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.Journal of medicinal chemistry, , Apr-26, Volume: 44, Issue:9, 2001
(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 diacJournal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.Journal of medicinal chemistry, , Apr-26, Volume: 44, Issue:9, 2001
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , May-05, Volume: 8, Issue:9, 1998
Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 19, Issue:9, 2010
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| beta-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of beta-adrenergic receptors; the activity involves transmitting the signal to the Gs alpha subunit of a heterotrimeric G protein. [GOC:cb, GOC:mah, IUPHAR_GPCR:1274] |
| beta1-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of beta1-adrenergic receptors. [GOC:mah, IUPHAR_GPCR:1274] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| PDZ domain binding | molecular function | Binding to a PDZ domain of a protein, a domain found in diverse signaling proteins. [GOC:go_curators, Pfam:PF00595] |
| alpha-2A adrenergic receptor binding | molecular function | Binding to an alpha-2A adrenergic receptor. [GOC:mah, GOC:nln] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potential | molecular function | A G protein-coupled neurotransmitter receptor activity, occurring in the postsynaptic membrane, involved in regulation of postsynaptic membrane potential. [GOC:dos] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| early endosome | cellular component | A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| Schaffer collateral - CA1 synapse | cellular component | A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689] |
| neuronal dense core vesicle | cellular component | A dense core vesicle (granule) that is part of a neuron. These vesicles typically contain neuropeptides. They can be found in all parts of neurons, including the soma, dendrites, axonal swellings (varicosities) and synaptic terminals. [GOC:dos, ISBN:978-0-07-181001-2, Wikipedia:Neuropeptide&oldid=713905176] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 14 target(s):
| Target | Category | Definition |
|---|
| positive regulation of heart rate by epinephrine-norepinephrine | biological process | The process in which the presence of epinephrine or norepinephrine in the bloodstream activates, maintains or increases the rate of heart contraction. [GOC:dph] |
| positive regulation of the force of heart contraction by epinephrine-norepinephrine | biological process | Any process that increases the force with which the cardiac muscles of the heart pump blood through the circulatory system as a result of the presence of epinephrine or norepinephrine in the bloodstream or released from the nerve endings. [GOC:dph, GOC:mtg_cardio] |
| diet induced thermogenesis | biological process | The process that results in increased metabolic rate in tissues of an organism. It is triggered by the detection of dietary excess. This process is achieved via signaling in the sympathetic nervous system. [PMID:12161655] |
| response to cold | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cold stimulus, a temperature stimulus below the optimal temperature for that organism. [GOC:lr] |
| heat generation | biological process | Any homeostatic process in which an organism produces heat, thereby raising its internal temperature. [GOC:mah] |
| negative regulation of multicellular organism growth | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of growth of an organism to reach its usual body size. [GOC:dph, GOC:ems, GOC:tb] |
| fear response | biological process | The response of an organism to a perceived external threat. [GOC:go_curators] |
| regulation of circadian sleep/wake cycle, sleep | biological process | Any process that modulates the frequency, rate or extent of sleep; a readily reversible state of reduced awareness and metabolic activity that occurs periodically in many animals. [GOC:jl, ISBN:0192800981] |
| brown fat cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a brown adipocyte, an animal connective tissue cell involved in adaptive thermogenesis. Brown adipocytes contain multiple small droplets of triglycerides and a high number of mitochondria. [PMID:12588810] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |
| positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | biological process | A process that results in an increase in the diameter of an artery during the norepinephrine-epinephrine response to blood pressure change. [GOC:mtg_cardio, PMID:10358008] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |