FR 113680
Names
[ CAS No. ]:
126088-92-4
[ 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]:
[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]
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