FR 113680

Names

[ Name ]:
FR 113680

[Synonym ]:
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)

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.26g/cm3

[ Molecular Formula ]:
C₃₅H₃₉N₅O₆

[ Molecular Weight ]:
625.71

[ Exact Mass ]:
625.29000

[ PSA ]:
158.53000

[ LogP ]:
4.20270

[ Index of Refraction ]:
1.624

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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