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4-(4-(2-(3-(2-氨基乙基)-1H-吲哚-5-基氧基)乙酰基)哌嗪-1-基)苯甲腈盐酸盐

用途

Donitriptan hydrochloride (F-11356) 是一种有效的高亲和力 5-HT1B/1D 受体激动剂,pKi 分别为 9.4 和 9.3。

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名称

[ CAS 号 ]:
170911-68-9

[ 中文名 ]:
4-(4-(2-(3-(2-氨基乙基)-1H-吲哚-5-基氧基)乙酰基)哌嗪-1-基)苯甲腈盐酸盐

[ 英文名 ]:
Donitriptan monohydrochloride

[英文别名 ]:

Donitriptan hydrochloride
Donitriptan monohydrochloride
Nafadotride

生物活性

[ 描述 ]:

Donitriptan hydrochloride (F-11356) 是一种有效的高亲和力 5-HT1B/1D 受体激动剂,pKi 分别为 9.4 和 9.3。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT1B Receptor:9.4 (pKi)

5-HT1D Receptor:9.3 (pKi)

[参考文献]

[1]. Muñoz-Islas E, et al. Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors. Br J Pharmacol. 2006 Sep;149(1):82-91.

物理化学性质

[ 沸点 ]:
727.1ºC at 760 mmHg

[ 分子式 ]:
C₂₃H₂₆ClN₅O₂

[ 分子量 ]:
439.94

[ 闪点 ]:
393.6ºC

[ 精确质量 ]:
439.17800

[ PSA ]:
98.38000

[ LogP ]:
3.77358

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
5.34E-21mmHg at 25°C

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H312-H315-H319-H332-H335

[ 警示性声明 ]:
P261-P280-P301 + P310-P305 + P351 + P338

[ 危险品运输编码 ]:
UN 3439 6.1 / PGIII

文献

Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors.

Br. J. Pharmacol. 149(1) , 82-91, (2006)

It has been suggested that during a migraine attack capsaicin-sensitive trigeminal sensory nerves release calcitonin gene-related peptide (CGRP), resulting in cranial vasodilatation and central nocice...

Donitriptan (Pierre Fabre).

Curr. Opin. Investig. Drugs 2(3) , 415-8, (2001)

Pierre Fabre is developing donitriptan, a piperazide 5-HT1D agonist, as a potential treatment for migraine [175854]. In January 2001, donitriptan had completed phase I trials for migraine and was sche...

Effects of donitriptan on carotid haemodynamics and cardiac output distribution in anaesthetized pigs.

Cephalalgia 22(1) , 37-47, (2002)

We investigated the effects of donitriptan, which possesses a uniquely high affinity and efficacy at 5-HT1B/1D receptors, on carotid and systemic haemodynamics in anaes thetized pigs. Donitriptan (0.1...

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