Bioactivity | FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1]. |
Invitro | 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: |
Name | FR 113680 |
CAS | 126088-92-4 |
Sequence | Ac-Thr-{d-Trp(For)}-{Phe(NMe,Bzl)} |
Shortening | Ac-T-{d-Trp(For)}-{Phe(NMe,Bzl)} |
Formula | C35H39N5O6 |
Molar Mass | 625.71 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |