163727-74-0

163727-74-0 structure

Name: WIN 64338 hydrochloride
Chemical Name: (S)-4-[2-[Bis(cyclohexylamino)methyleneamino]-3-(2-naphthalenyl)-1-oxopropylamino]benzyl tributyl phosphonium chloride hydrochloride
CAS Number: 163727-74-0
Molecular Formula: C₄₅H₆₉Cl₂N₄OP
Molecular Weight: 783.935
Catalog: Signaling Pathways GPCR/G Protein Bradykinin Receptor
Create Date: 2021-01-09 18:03:34
Modify Date: 2024-01-13 11:44:00
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM)[1][2].

Name	(S)-4-[2-[Bis(cyclohexylamino)methyleneamino]-3-(2-naphthalenyl)-1-oxopropylamino]benzyl tributyl phosphonium chloride hydrochloride
Synonyms	(S)-4-[2-[Bis(cyclohexylamino)methyleneamino]-3-(2-naphthalenyl)-1-oxopropylamino]benzyl tributyl phosphonium chloride hydrochloride Phosphonium, tributyl[[4-[[(2S)-2-[[(E)-(cyclohexylamino)(cyclohexylimino)methyl]amino]-3-(2-naphthalenyl)-1-oxopropyl]amino]phenyl]methyl]-, chloride, hydrochloride (1:1:1) N2-(N,N'-Dicyclohexylcarbamimidoyl)-3-(2-naphthyl)-N-{4-[(tributylphosphonio)methyl]phenyl}-L-alaninamide chloride hydrochloride (1:1:1) phosphonium, tributyl[[4-[[(2S)-2-[[(E)-(cyclohexylamino)(cyclohexyliminio)methyl]amino]-3-(2-naphthalenyl)-1-oxopropyl]amino]phenyl]methyl]-, chloride (1:2)

Description	WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM)[1][2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> mAChR Signaling Pathways >> GPCR/G Protein >> mAChR Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Bradykinin Receptor
Target	Ki: 64 nM (bradykinin B2 receptor)[1], 350 nM (muscarinic receptor)[2]
In Vitro	WIN 64338 hydrochloride competitively inhibits Bradykinin-stimulated 45Ca2+ efflux from IMR-90 cells (pA2=7.1)[1]. WIN 64338 hydrochloride inhibits Bradykinin-mediated guinea pig ileum contractility (pA2=8.2)[1]. WIN 64338 hydrochloride inhibits Bradykinin-induced contraction of guinea-pig trachea, with a KB of 64.3 nM[2].
In Vivo	WIN 64338 (5 mg/kg; i.p.) hydrochloride decreases the physiological anxiety measure, stress-induced hyperthermia (SIH) of mice[3].
References	[1]. Sawutz DG, et, al. The nonpeptide WIN 64338 is a bradykinin B2 receptor antagonist. Proc Natl Acad Sci U S A. 1994 May 24;91(11):4693-7. [2]. Scherrer D, et, al. Effects of WIN 64338, a nonpeptide bradykinin B2 receptor antagonist, on guinea-pig trachea. Br J Pharmacol. 1995 Aug;115(7):1127-8. [3]. Rouhiaine A, et, al. The bradykinin system in stress and anxiety in humans and mice. Sci Rep. 2019 Dec 19;9(1):19437.

Molecular Formula	C₄₅H₆₉Cl₂N₄OP
Molecular Weight	783.935
Exact Mass	782.458618

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