L-371,257 |
カタログ番号GC11991 |
L-371,257 は、オキシトシン受容体 (Ki = 19 nM) とバソプレシン V1a 受容体 (Ki = 3.7) の両方に高い親和性を持つ、オキシトシン受容体 (pA2 = 8.4) の選択的かつ競合的なアンタゴニストです。 nM)。
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Cas No.: 162042-44-6
Sample solution is provided at 25 µL, 10mM.
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM)[1][2].
References:
[1]. Williams PD, et al. 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. J Med Chem. 1995 Nov 10;38(23):4634-6.
[2]. Tunstall BJ, et al. Oxytocin blocks enhanced motivation for alcohol in alcohol dependence and blocks alcohol effects on GABAergic transmission in the central amygdala. PLoS Biol. 2019 Apr 16;17(4):e2006421.
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