126088-92-4

126088-92-4 structure

Name: FR 113680
Chemical Name: (2S,3R)-2-acetamido-N-[(2R)-2-amino-3-(1-formylindol-3-yl)propanoyl]-N-[(2S)-2-[benzyl(methyl)amino]-3-phenylpropanoyl]-3-hydroxybutanamide
CAS Number: 126088-92-4
Molecular Formula: C₃₅H₃₉N₅O₆
Molecular Weight: 625.71
Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
Create Date: 2016-08-20 20:55:33
Modify Date: 2024-01-26 17:39:24
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1].

Name	(2S,3R)-2-acetamido-N-[(2R)-2-amino-3-(1-formylindol-3-yl)propanoyl]-N-[(2S)-2-[benzyl(methyl)amino]-3-phenylpropanoyl]-3-hydroxybutanamide
Synonyms	Ac-Thr-D-Trp(CHO)-Phe-NMeBzl Ac-Thr-trp(cho)-phe-N-mebzl L-Phenylalaninamide,N-acetyl-L-threonyl-1-formyl-D-tryptophyl-N-methyl-N-(phenylmethyl)

Description	FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor
In Vitro	FR 113680 对 SP 诱导的豚鼠回肠收缩具有竞争性抑制作用，pA2 值为 7.53[1]。 FR 113680 对 [3H]-SP 结合大鼠大脑皮质膜 (NK1)、[3H]-神经激肽 A ([3H]-NKA) 结合大鼠十二指肠平滑肌膜 (NK2) 和 [3H]-eledoisin (Ele) 结合大鼠大脑皮质膜 (NK3) 无影响[1]。
In Vivo	FR 113680 (32 mg/kg; i.v.; once) 显著抑制香烟烟雾引起的血浆外渗[2]。 Animal Model: Male Wistar rats, cigarette smoke-induced rat tracheal plasma extravasation model[2] Dosage: 0, 10 and 32 mg/kg Administration: IV, once Result: Significantly inhibited cigarette smoke-induced rat tracheal plasma extravasation at a dose of 32 mg/kg.
References	[1]. Morimoto H, et al. FR 113680: a novel tripeptide substance P antagonist with NK1 receptor selectivity. Br J Pharmacol. 1992 May;106(1):123-6. [2]. Morimoto H, et al. Effects of FR 113680 and FK 224, novel tachykinin receptor antagonists, on cigarette smoke-induced rat tracheal plasma extravasation. Eur J Pharmacol. 1992 Nov 24;224(1):1-5.

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