solabegron profile

solabegron: GW-427353 is the (R)-isomer; [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

solabegron : A carboxybiphenyl that is [biphenyl]-3-carboxylic acid carrying a (2-{[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}ethyl)nitrilo group at the 3' position. A selective beta3-adrenergic receptor agonist currently in clinical development for the treatment of overactive bladder and irritable bowel syndrome. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	9887812
CHEMBL ID	208427
CHEBI ID	141346
SCHEMBL ID	2596555
MeSH ID	M0515159

Synonym
CHEMBL208427
gw427353
(r)-3'-((2-((2-(3-chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)-(1,1'-biphenyl)-3-carboxylic acid
252920-94-8
CHEBI:141346
solabegron
3'-[(2-{[(2r)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}ethyl)amino][biphenyl]-3-carboxylic acid
gw 427353
gw-427353
solabegronum
(r)-3'-((2-((2-(3-chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)-[1,1'-biphenyl]-3-carboxylic acid
AKOS016003955
solabegron [inn]
(1,1'-biphenyl)-3-carboxylic acid, 3'-((2-(((2r)-2-(3-chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)-
unii-55p6yh9o6n
55p6yh9o6n ,
(r)-3'-[[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]amino]ethyl]amino]-[1,1'-biphenyl]-3-carboxylic acid
(r)-3'-(2-(2-(3-chlorophenyl)-2-hydroxyethylamino)ethylamino)biphenyl-3-carboxylic acid
LLDXOPKUNJTIRF-QFIPXVFZSA-N
solabegron [who-dd]
3'-((2-(((2r)-2-(3-chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)biphenyl-3-carboxylic acid
SCHEMBL2596555
bdbm50002595
DTXSID50179932
3'-[(2-{[(2r)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}ethyl)amino]-[1,1'-biphenyl]-3-carboxylic acid
AS-74724
compound 38 [pmid: 16640337]
3-[3-[2-[[(2r)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]ethylamino]phenyl]benzoic acid
gtpl9512
DB06190
[1,1'-biphenyl]-3-carboxylicacid,3'-[[2-[[(2r)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]ethyl]amino]-
HY-19436
CS-0015536
solabegron (hydrochloride)
D93408
gw 427353gw 427353
solabegron-13c6
CKA92094

Excerpt	Reference	Relevance
"Solabegron 125 mg treatment also showed statistically significant reductions from baseline to weeks 4 and 8 in micturitions over 24 h and a statistically significant increase from baseline to week 8 in urine volume voided."	( A multicenter, double-blind, randomized, placebo-controlled trial of the β3-adrenoceptor agonist solabegron for overactive bladder. Michel, MC; Ohlstein, EH; von Keitz, A, 2012)	1.32

Excerpt	Reference	Relevance
"Based on a systematic PubMed search, incidence of overall adverse events, hypertension, dry mouth, and constipation are comparable between mirabegron or solabegron and placebo."	( Safety and tolerability of β3-adrenoceptor agonists in the treatment of overactive bladder syndrome - insight from transcriptosome and experimental studies. Gravas, S; Michel, MC, 2016)	0.63
" We propose that expression profiles and functional preclinical studies can be important tools in the prediction of adverse event profiles in first-in-class drugs."	( Safety and tolerability of β3-adrenoceptor agonists in the treatment of overactive bladder syndrome - insight from transcriptosome and experimental studies. Gravas, S; Michel, MC, 2016)	0.43

Excerpt	Reference	Relevance
"A novel class of biphenyl analogues containing a benzoic acid moiety based on lead compound 8i have been identified as potent and selective human beta 3 adrenergic receptor (beta 3-AR) agonists with good oral bioavailability and long plasma half-life."	( 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. Hamada, K; Hamashima, H; Hattori, K; Imamura, E; Imanishi, M; Ishikawa, H; Itou, S; Matsui, S; Matsumura, Y; Nakajima, Y; Nakano, K; Sakurai, M; Takamura, F; Tomishima, Y; Ueshima, K; Unami, N; Washizuka, K; Yamamoto, N; Yamamoto, T, 2008)	0.35

Role	Description
beta-adrenergic agonist	An agent that selectively binds to and activates beta-adrenergic receptors.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
secondary alcohol	A secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
substituted aniline
monochlorobenzenes	Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
secondary amino compound	A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
carboxybiphenyl	Any member of the class of biphenyls that has one or more carboxy groups attached to the biphenyl skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Beta-2 adrenergic receptor	Homo sapiens (human)	Ki	1.5849	0.0000	0.6635	9.5499	AID264428
Beta-1 adrenergic receptor	Homo sapiens (human)	Ki	0.3981	0.0001	1.3391	9.9840	AID264430
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Beta-2 adrenergic receptor	Homo sapiens (human)	EC50 (µMol)	1.2589	0.0000	0.3111	10.0000	AID264375
Beta-1 adrenergic receptor	Homo sapiens (human)	EC50 (µMol)	3.9811	0.0001	0.4914	6.0000	AID264377
Beta-3 adrenergic receptor	Homo sapiens (human)	EC50 (µMol)	0.0040	0.0001	0.4553	10.0000	AID264374
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
diet induced thermogenesis	Beta-2 adrenergic receptor	Homo sapiens (human)
regulation of sodium ion transport	Beta-2 adrenergic receptor	Homo sapiens (human)
transcription by RNA polymerase II	Beta-2 adrenergic receptor	Homo sapiens (human)
receptor-mediated endocytosis	Beta-2 adrenergic receptor	Homo sapiens (human)
smooth muscle contraction	Beta-2 adrenergic receptor	Homo sapiens (human)
cell surface receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activity	Beta-2 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
endosome to lysosome transport	Beta-2 adrenergic receptor	Homo sapiens (human)
response to cold	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of protein kinase A signaling	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of bone mineralization	Beta-2 adrenergic receptor	Homo sapiens (human)
heat generation	Beta-2 adrenergic receptor	Homo sapiens (human)
negative regulation of multicellular organism growth	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Beta-2 adrenergic receptor	Homo sapiens (human)
bone resorption	Beta-2 adrenergic receptor	Homo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Beta-2 adrenergic receptor	Homo sapiens (human)
negative regulation of smooth muscle contraction	Beta-2 adrenergic receptor	Homo sapiens (human)
brown fat cell differentiation	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of mini excitatory postsynaptic potential	Beta-2 adrenergic receptor	Homo sapiens (human)
adrenergic receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of protein serine/threonine kinase activity	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of autophagosome maturation	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of lipophagy	Beta-2 adrenergic receptor	Homo sapiens (human)
cellular response to amyloid-beta	Beta-2 adrenergic receptor	Homo sapiens (human)
response to psychosocial stress	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of cAMP-dependent protein kinase activity	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of AMPA receptor activity	Beta-2 adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	Beta-2 adrenergic receptor	Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrine	Beta-1 adrenergic receptor	Homo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrine	Beta-1 adrenergic receptor	Homo sapiens (human)
diet induced thermogenesis	Beta-1 adrenergic receptor	Homo sapiens (human)
response to cold	Beta-1 adrenergic receptor	Homo sapiens (human)
heat generation	Beta-1 adrenergic receptor	Homo sapiens (human)
negative regulation of multicellular organism growth	Beta-1 adrenergic receptor	Homo sapiens (human)
fear response	Beta-1 adrenergic receptor	Homo sapiens (human)
regulation of circadian sleep/wake cycle, sleep	Beta-1 adrenergic receptor	Homo sapiens (human)
brown fat cell differentiation	Beta-1 adrenergic receptor	Homo sapiens (human)
regulation of postsynaptic membrane potential	Beta-1 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Beta-1 adrenergic receptor	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Beta-1 adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	Beta-1 adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Beta-1 adrenergic receptor	Homo sapiens (human)
receptor-mediated endocytosis	Beta-3 adrenergic receptor	Homo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathway	Beta-3 adrenergic receptor	Homo sapiens (human)
diet induced thermogenesis	Beta-3 adrenergic receptor	Homo sapiens (human)
carbohydrate metabolic process	Beta-3 adrenergic receptor	Homo sapiens (human)
generation of precursor metabolites and energy	Beta-3 adrenergic receptor	Homo sapiens (human)
energy reserve metabolic process	Beta-3 adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Beta-3 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Beta-3 adrenergic receptor	Homo sapiens (human)
response to cold	Beta-3 adrenergic receptor	Homo sapiens (human)
heat generation	Beta-3 adrenergic receptor	Homo sapiens (human)
negative regulation of multicellular organism growth	Beta-3 adrenergic receptor	Homo sapiens (human)
eating behavior	Beta-3 adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Beta-3 adrenergic receptor	Homo sapiens (human)
brown fat cell differentiation	Beta-3 adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Beta-3 adrenergic receptor	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Beta-3 adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	Beta-3 adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
amyloid-beta binding	Beta-2 adrenergic receptor	Homo sapiens (human)
beta2-adrenergic receptor activity	Beta-2 adrenergic receptor	Homo sapiens (human)
protein binding	Beta-2 adrenergic receptor	Homo sapiens (human)
adenylate cyclase binding	Beta-2 adrenergic receptor	Homo sapiens (human)
potassium channel regulator activity	Beta-2 adrenergic receptor	Homo sapiens (human)
identical protein binding	Beta-2 adrenergic receptor	Homo sapiens (human)
protein homodimerization activity	Beta-2 adrenergic receptor	Homo sapiens (human)
protein-containing complex binding	Beta-2 adrenergic receptor	Homo sapiens (human)
norepinephrine binding	Beta-2 adrenergic receptor	Homo sapiens (human)
beta-adrenergic receptor activity	Beta-1 adrenergic receptor	Homo sapiens (human)
beta1-adrenergic receptor activity	Beta-1 adrenergic receptor	Homo sapiens (human)
protein binding	Beta-1 adrenergic receptor	Homo sapiens (human)
PDZ domain binding	Beta-1 adrenergic receptor	Homo sapiens (human)
alpha-2A adrenergic receptor binding	Beta-1 adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Beta-1 adrenergic receptor	Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potential	Beta-1 adrenergic receptor	Homo sapiens (human)
norepinephrine binding	Beta-3 adrenergic receptor	Homo sapiens (human)
beta-adrenergic receptor activity	Beta-3 adrenergic receptor	Homo sapiens (human)
protein binding	Beta-3 adrenergic receptor	Homo sapiens (human)
beta3-adrenergic receptor activity	Beta-3 adrenergic receptor	Homo sapiens (human)
beta-3 adrenergic receptor binding	Beta-3 adrenergic receptor	Homo sapiens (human)
protein homodimerization activity	Beta-3 adrenergic receptor	Homo sapiens (human)
epinephrine binding	Beta-3 adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleus	Beta-2 adrenergic receptor	Homo sapiens (human)
lysosome	Beta-2 adrenergic receptor	Homo sapiens (human)
endosome	Beta-2 adrenergic receptor	Homo sapiens (human)
early endosome	Beta-2 adrenergic receptor	Homo sapiens (human)
Golgi apparatus	Beta-2 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
endosome membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
apical plasma membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
clathrin-coated endocytic vesicle membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
neuronal dense core vesicle	Beta-2 adrenergic receptor	Homo sapiens (human)
receptor complex	Beta-2 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-2 adrenergic receptor	Homo sapiens (human)
early endosome	Beta-1 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-1 adrenergic receptor	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Beta-1 adrenergic receptor	Homo sapiens (human)
neuronal dense core vesicle	Beta-1 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-1 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-3 adrenergic receptor	Homo sapiens (human)
receptor complex	Beta-3 adrenergic receptor	Homo sapiens (human)
plasma membrane	Beta-3 adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay ID	Title	Year	Journal	Article
AID1346260	Human beta1-adrenoceptor (Adrenoceptors)	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID1346250	Human beta2-adrenoceptor (Adrenoceptors)	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID1346297	Human beta3-adrenoceptor (Adrenoceptors)	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264378	Selectivity for human beta-3 adrenergic receptor over beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264397	Decrease in glycosylated hemoglobin in db/db mouse at 30 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264433	Activity against human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production relative to R-(-)-isoproterenol	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264412	Increase of thermogenic activity in CD1 mouse at 10 mg/kg	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264374	Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264405	Decrease in plasma insulin level in db/db mouse at 10 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID317593	Half life in dog	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	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.
AID264382	Half life in po dosed Beagle dog	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264428	Displacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cells	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264417	Half life in Wistar Han rat at 1 mg/kg, iv	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264434	Activity against human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production relative to R-(-)-isoproterenol	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264425	Half life in iv dosed cynomolgus monkey	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264416	Volume of distribution in Wistar Han rat at 1 mg/kg, iv or 1 mg/kg, po	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264383	Bioavailability in Beagle dog	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264379	AUC(0-infinity) in po dosed Beagle dog	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264381	Volume of distribution in Beagle dog	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID317594	Half life in monkey	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	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.
AID264380	Clearance in Beagle dog	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264415	Renal clearance in Wistar Han rat at 1 mg/kg, iv or 1 mg/kg, po	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264413	Increase of thermogenic activity in CD1 mouse at 30 mg/kg	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID317589	Oral bioavailability in rat	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	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.
AID264418	Half life in Wistar Han rat at 1 mg/kg, po	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264376	Selectivity for human beta3 adrenergic receptor over beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264419	Bioavailability in Wistar Han rat at 1 mg/kg, po and 1 mg/kg, iv	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264388	Decrease in plasma glucose level in db/db mouse at 30 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID317590	Oral bioavailability in dog	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	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.
AID317592	Half life in rat	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	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.
AID264427	Bioavailability in cynomolgus monkey	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264424	Volume of distribution in cynomolgus monkey	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264421	Half life in Beagle dog at 0.2 mg/kg, iv	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264420	Renal clearance in Beagle dog	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264411	Increase of thermogenic activity in CD1 mouse at 3 mg/kg	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264396	Decrease in glycosylated hemoglobin in db/db mouse at 10 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264432	Activity against human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production relative to R-(-)-isoproterenol	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264414	Clearance in Wistar Han rat at 1 mg/kg, iv or 1 mg/kg, po	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264406	Decrease in plasma insulin level in db/db mouse at 30 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264387	Decrease in plasma glucose level in db/db mouse at 10 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264422	Clearance in cynomolgus monkey	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264430	Displacement of [125I]cyanopindolol from human cloned beta-1 adrenergic receptor expressed in Sf9 cells	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264389	Decrease in plasma glucose level in db/db mouse at 100 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264431	Ratio of pEC50 for human beta-3 adrenergic receptor to pKi for human beta-1 adrenergic receptor	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264398	Decrease in glycosylated hemoglobin in db/db mouse at 100 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264375	Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264429	Ratio of pEC50 for human beta-3 adrenergic receptor to pKi for human beta2 adrenergic receptor	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264407	Decrease in plasma insulin level in db/db mouse at 100 mg/kg, po after 14 days	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264377	Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID317591	Oral bioavailability in monkey	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	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.
AID264423	Renal clearance in cynomolgus monkey	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
AID264426	Half life in po dosed cynomolgus monkey	2006	Journal of medicinal chemistry, May-04, Volume: 49, Issue:9	Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (25.00)	29.6817
2010's	10 (62.50)	24.3611
2020's	2 (12.50)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (11.76%)	5.53%
Reviews	4 (23.53%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (64.71%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Phase 2b, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study to Evaluate the Efficacy and Safety of Oral Solabegron Immediate Release Tablets in the Treatment of Overactive Bladder (OAB) in Adult Female Subjects [NCT03475706]	Phase 2	438 participants (Actual)	Interventional	2018-02-19	Completed
A Randomized, Double-Blind, Placebo-Controlled, Crossover, Phase IIa Study to Evaluate Efficacy and Safety of the Beta-3-Adrenergic Receptor Agonist Solabegron in Subjects With Irritable Bowel Syndrome [NCT00394186]	Phase 2	100 participants (Actual)	Interventional	2006-08-31	Completed
A Randomized, Repeat Dose Study to Investigate the Pharmacokinetics, Safety and Tolerability of Solabegron (GW427353) in Combination With Oxybutynin in Healthy Adult Subjects. [NCT00501267]	Phase 1	24 participants (Actual)	Interventional	2007-06-30	Completed
A Two-Part Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Four MR Formulations and Food Effect of GW427353 (Solabegron) in Healthy Adult Subjects [NCT00427596]	Phase 1	18 participants (Actual)	Interventional	2007-01-31	Completed
An Eight- Week Randomized, Double-Blind, Placebo-Controlled, Parallel Group Proof of Concept Study to Assess the Efficacy, Safety and Tolerability as Well as the Pharmacokinetic Profile of Oral Solabegron (GW427353) 125mg and 50mg Administered Twice Daily [NCT00343486]	Phase 2	240 participants	Interventional	2006-05-31	Completed
A Phase 1 Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Immediate and Modified Release Formulations of Orally Administered Solabegron in Healthy Male Subjects [NCT02938507]	Phase 1	24 participants (Actual)	Interventional	2016-10-31	Completed
An Exploratory Phase I Study in Healthy Volunteers of GI Transit Following Administration of the ß3-Adrenergic Receptor Agonist, Solabegron (Study B3I106248) [NCT00401479]	Phase 1	36 participants (Actual)	Interventional	2006-10-31	Completed
A Phase 2b, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study to Evaluate the Efficacy and Safety of Oral Solabegron Modified Release Tablets in the Treatment of Overactive Bladder (OAB) in Adult Female Subjects [NCT03594058]	Phase 2	1,413 participants (Actual)	Interventional	2018-07-09	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Substance	Relationship Strength	Studies	Classes	Roles
acetic acid Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed). acetic acid : A simple monocarboxylic acid containing two carbons.	2.03	1	monocarboxylic acid	antimicrobial food preservative; Daphnia magna metabolite; food acidity regulator; protic solvent
isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.	2.77	3	catechols; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.07	1	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
thiazoles [no description available]	5.87	4	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.	2.05	1	3-(1-methylpyrrolidin-2-yl)pyridine	anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic
amibegron [no description available]	2.07	1	monocarboxylic acid
ritobegron [no description available]	2.6	1
mirabegron mirabegron: a beta3-adrenergic receptor agonist; structure in first source. mirabegron : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-amino-1,3-thiazol-4-ylacetic acid with the anilino group of (1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethanol. Used for the treatment of overactive bladder syndrome.	6.08	5	1,3-thiazoles; aromatic amide; ethanolamines; monocarboxylic acid amide	beta-adrenergic agonist
sr 59230a 3-(2-ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate: structure given in first source	2.05	1

Condition	Indicated	Relationship Strength	Studies	Trials
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	0	2.04	1	0
Diabetes Mellitus, Adult-Onset [description not available]	0	2.41	1	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	0	2.41	1	0
Bladder, Overactive [description not available]	0	10.43	10	4
Urinary Bladder, Overactive Symptom of overactive detrusor muscle of the URINARY BLADDER that contracts with abnormally high frequency and urgency. Overactive bladder is characterized by the frequent feeling of needing to urinate during the day, during the night, or both. URINARY INCONTINENCE may or may not be present.	1	12.43	10	4
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	3.96	1	0
Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position.	0	2.46	2	0
Urinary Incontinence Involuntary loss of URINE, such as leaking of urine. It is a symptom of various underlying pathological processes. Major types of incontinence include URINARY URGE INCONTINENCE and URINARY STRESS INCONTINENCE.	0	7.68	5	4
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.03	1	0
Bilateral Headache [description not available]	0	3.43	1	1
Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.	0	3.43	1	1

solabegron

Description

Cross-References

Synonyms (38)

Research Excerpts

Treatment

Toxicity

Bioavailability

Roles (1)

Drug Classes (5)

Protein Targets (3)

Inhibition Measurements

Activation Measurements

Biological Processes (42)

Molecular Functions (18)

Ceullar Components (13)

Bioassays (52)

Research

Studies (16)

Market Indicators

Research Demand Index: 35.23

Study Types

Clinical Trials (8)

Trial Overview

solabegron

Description

Cross-References

Synonyms (38)

Research Excerpts

Treatment

Toxicity

Bioavailability

Roles (1)

Drug Classes (5)

Protein Targets (3)

Inhibition Measurements

Activation Measurements

Biological Processes (42)

Molecular Functions (18)

Ceullar Components (13)

Bioassays (52)

Research

Studies (16)

Market Indicators

Research Demand Index: 35.23

Study Types

Clinical Trials (8)

Trial Overview

Related Drugs (9)

Related Conditions (11)