Compounds > sb 236057
Page last updated: 2024-11-10

sb 236057

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

SB 236057: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311426
CHEMBL ID1628625
SCHEMBL ID7831487
MeSH IDM0334657

Synonyms (25)

Synonym
gtpl3231
sb 236057
1'-ethyl-7-({4-[2-methyl-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]phenyl}carbonyl)-2,5,6,7-tetrahydrospiro[furo[2,3-f]indole-1,4'-piperidine]
sb236057
L000541
(1'-ethylspiro[6,7-dihydro-2h-furo[2,3-f]indole-3,4'-piperidine]-5-yl)-[4-[2-methyl-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]phenyl]methanone
sb-236057
CHEMBL1628625
NCGC00247934-01
DTXSID0047321
180083-49-2
(1'-ethyl-6,7-dihydro-5h-spiro[furo[2,3-f]indole-3,4'-piperidin]-5-yl)[2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-yl]methanone
1'-ethyl-5-[2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine]
WXAKEEQOWUHGCI-UHFFFAOYSA-N ,
SCHEMBL7831487
(1'-ethyl-6,7-dihydro-2h,5h-spiro[furo[2,3-f]indole-3,4'-piperidin]-5-yl)(2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)-[1,1'-biphenyl]-4-yl)methanone
Q21098842
methanone, (1'-ethyl-2,5,6,7-tetrahydrospiro[3h-furo[2,3-f]indole-3,4'-piperidin]-5-yl)[2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)[1,1'-biphenyl]-4-yl]-
spiro[2h-furo[2,3-f]indole-3(5h),4'-piperidine], 1'-ethyl-6,7-dihydro-5-[[2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)[1,1'-biphenyl]-4-yl]carbonyl]-
methanone, (1'-ethyl-2,5,6,7-tetrahydrospiro(3h-furo(2,3-f)indole-3,4'-piperidin)-5-yl)(2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)(1,1'-biphenyl)-4-yl)-
spiro(2h-furo(2,3-f)indole-3(5h),4'-piperidine), 1'-ethyl-6,7-dihydro-5-((2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)(1,1'-biphenyl)-4-yl)carbonyl)-
unii-6w25pbe4md
6w25pbe4md ,
(1'-ethyl-6,7-dihydro-5h-spiro(furo(2,3-f)indole-3,4'-piperidin)-5-yl)(2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-yl)methanone
AKOS040749421

Research Excerpts

Effects

ExcerptReferenceRelevance
"SB 236057-A has been shown to have high affinity for human 5-HT1B receptors (pK(i) = 8.2) and displays 80 or more fold selectivity for the human 5-HT1B receptor over other 5-HT receptors and a range of additional receptors, ion channels and enzymes."( SB-236057-A: a selective 5-HT1B receptor inverse agonist.
Middlemiss, DN; Price, GW; Roberts, C; Watson, J, 2001)		1.03

Bioavailability

ExcerptReferenceRelevance
" 23% bioavailability following oral drug administration."( The effect of SB-236057-A, a selective 5-HT1B receptor inverse agonist, on in vivo extracellular 5-HT levels in the freely-moving guinea-pig.
Austin, NE; Gaster, LM; Hagan, JJ; Hatcher, P; Jeffrey, P; Middlemiss, DN; Roberts, C; Routledge, C; Wyman, P, 2000)		0.31

Dosage Studied

ExcerptRelevanceReference
" Dams were then dosed on days 8-11 pc and embryos were evaluated by histochemical procedures on days 11, 13, or 15 pc."( SB-236057: Critical window of sensitivity study and embryopathy of a potent musculoskeletal teratogen.
Augustine-Rauch, KA; DeBoer, LS; Mirabile, R; Posobiec, L; Solomon, HM; Wier, PJ; Zhang, QJ, 2004)		0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Jun-30, Volume: 375, Issue:1-3
SB-236057, a selective 5-HT1B receptor inverse agonist, blocks the 5-HT human terminal autoreceptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (20.00)18.2507
2000's4 (80.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.66

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.66 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		210sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		3.110aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.4220
Abnormalities, Musculoskeletal
[description not available]		02.0210
Hypothermia, Accidental
[description not available]		03.3220
Hypothermia
Lower than normal body temperature, especially in warm-blooded animals.		03.3220