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WIN 64338 hydrochloride

Names

[ CAS No. ]:
163727-74-0

[ Name ]:
WIN 64338 hydrochloride

[Synonym ]:
(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)

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C45H69Cl2N4OP

[ Molecular Weight ]:
783.935

[ Exact Mass ]:
782.458618

Related Compounds