Page last updated: 2024-12-08

repinotan hydrochloride

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

Description

repinotan hydrochloride: 5-HT(1A) receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID198756
MeSH IDM0288093

Synonyms (22)

Synonym
bay-x-3702
repinotan hydrochloride
x-3702 ,
branosyn
bay x 3702
1,2-benzisothiazol-3(2h)-one, 2-(4-(((3,4-dihydro-2h-1-benzopyran-2-yl)methyl)amino)butyl)-, 1,1-dioxide, monohydrochloride, (-)-
(-)-(r)-2-(4-((chroman-2-ylmethyl)amino)butyl)-1,1-dioxo-1,2-benzisothiazol-3(2h)-one hcl
1kbq63168a ,
144980-77-8
repinotan hcl
unii-1kbq63168a
bayx3702
repinotan hydrochloride [mi]
IGKYREHZJIHPML-UNTBIKODSA-N
2-(4-{[(3,4-dihydro-2h-1-benzopyran-2-yl)methyl]amino}butyl)-1h-1lambda~6~,2-benzothiazole-1,1,3(2h)-trione--hydrogen chloride (1/1)
DTXSID70932465
2-[4-[[(2r)-3,4-dihydro-2h-chromen-2-yl]methylamino]butyl]-1,1-dioxo-1,2-benzothiazol-3-one;hydrochloride
Q27252535
MS-27832
repinotan (hydrochloride)
HY-12959A
AKOS040749285

Research Excerpts

Overview

Repinotan hydrochloride is a serotonin (5-HT)(1A) receptor full agonist with evidence of neuroprotection in animal models of focal ischemia. The effects on ventilation and nociception are unknown.

ExcerptReferenceRelevance
"Repinotan hydrochloride is a serotonin (5-HT)(1A) receptor full agonist with evidence of neuroprotection in animal models of permanent and transient focal ischemia. "( A randomized, double-blind, placebo-controlled trial to evaluate the efficacy, safety, tolerability, and pharmacokinetic/pharmacodynamic effects of a targeted exposure of intravenous repinotan in patients with acute ischemic stroke: modified Randomized Ex
Davis, S; Fierus, M; Hacke, W; Kaste, M; Lyden, PD; Teal, P, 2009
)
1.8
"Repinotan hydrochloride is a selective 5-HT(1A)-R-agonist already investigated in humans, but the effects on ventilation and nociception are unknown."( Repinotan, a selective 5-HT1A-R-agonist, antagonizes morphine-induced ventilatory depression in anesthetized rats.
Boettcher, MF; Guenther, U; Hoeft, A; Putensen, C; Theuerkauf, N; Wensing, G; Wrigge, H; Zinserling, J, 2010
)
1.08
"Repinotan hydrochloride (repinotan) is a highly potent and selective 5-HT(1A) full receptor agonist. "( Pharmacokinetics of repinotan in healthy and brain injured animals.
Beckermann, B; Buehner, K; Mauler, F; Schuhmacher, J; Schwarz, T; Seidel, D; Steinke, W; Weinz, C; Zimmerd, D, 2005
)
1.77

Toxicity

ExcerptReferenceRelevance
"Among 240 patients in the safety analysis, repinotan was well-tolerated, with adverse events appearing more frequently in the highest dose group (2."( The BRAINS study: safety, tolerability, and dose-finding of repinotan in acute stroke.
Silver, FL; Simard, D; Teal, P, 2005
)
0.33
"This study indicates that the incidence of adverse events was comparable with all doses of repinotan and placebo, and no safety issues were observed."( The BRAINS study: safety, tolerability, and dose-finding of repinotan in acute stroke.
Silver, FL; Simard, D; Teal, P, 2005
)
0.33

Dosage Studied

ExcerptRelevanceReference
" The favorable neuroprotective efficacy, broad dose-response curve, and prolonged therapeutic window observed in all models strongly suggest that repinotan is a promising candidate for treating acute ischemic stroke in humans."( Neuroprotective efficacy of repinotan HCl, a 5-HT1A receptor agonist, in animal models of stroke and traumatic brain injury.
Horváth, E; Mauler, F, 2005
)
0.33
"A dose-response curve of the repinotan effects on spontaneous minute ventilation during continuous remifentanil infusion in anesthetized rats was established to identify moderate doses: (1) tail-flick reflex latencies to assess nociception were recorded until 60 min after cessation of a continuous remifentanil infusion with or without a concomitant moderate repinotan dose (10 μg/kg), and (2) remifentanil boluses (2."( Selective 5-HT(1A)-R-agonist repinotan prevents remifentanil-induced ventilatory depression and prolongs antinociception.
Boettcher, MF; Guenther, U; Hoeft, A; Huse, D; Putensen, C; Theuerkauf, NU; Wensing, G, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's11 (31.43)18.2507
2000's22 (62.86)29.6817
2010's2 (5.71)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: 10.63

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 Index10.63 (24.57)
Research Supply Index3.69 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.63)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (11.43%)5.53%
Reviews3 (8.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other28 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-Blind, Placebo-Controlled Trial to Evaluate the Efficacy, Safety, Tolerability and Pharmacokinetic / Pharmacodynamic Effects of a Targeted Exposure of Intravenous Repinotan in Patients With Acute Ischemic Stroke [NCT00044915]Phase 2782 participants (Actual)Interventional2000-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]