FR 113680

Modify Date: 2024-01-26 17:39:24

FR 113680 Structure
FR 113680 structure
Common Name FR 113680
CAS Number 126088-92-4 Molecular Weight 625.71
Density 1.26g/cm3 Boiling Point N/A
Molecular Formula C35H39N5O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of FR 113680


FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1].

 Names

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
Synonym More Synonyms

 FR 113680 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

[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

~80%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

~%

FR 113680 Structure

FR 113680

CAS#:126088-92-4

Literature: Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

 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)
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