(+)-Norfenfluramine

立即咨询

(+)-Norfenfluramine

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

19036-73-8

(S)-1-(3-(三氟甲基)苯基)丙-2-胺

(+)-Norfenfluramine 是 (+)-fenfluramine 的主要肝脏代谢物，是一种选择性的5-HT_2B受体激动剂 (K_i: 11.2 nM)。(+)-Norfenfluramine 有效地刺激磷酸肌醇的水解并增加细胞内 Ca²⁺。(+)-Norfenfluramine 可用于原发性肺动脉高压和心脏瓣膜病的研究。

生物活性

(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective5-HT_2Breceptor agonist (K_i: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca²⁺. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease^[1].

IC₅₀& Target^[1]

5-HT_2BReceptor

11.2 nM (Ki)

5-HT_2AReceptor

1516 nM (Ki)

5-HT_2CReceptor

324 nM (Ki)

体外研究
(In Vitro)

(+)-Norfenfluramine (1 nM to 100 μM) contracts arteries with a dramatic decrease in threshold (aorta and mesenteric resistance artery) in rats^[1].
(+)-Norfenfluramine (1 and 10 μM, 3 min) induces contraction in aorta from tissues of normotensive and hypertensive rats^[1].
(+)-Norfenfluramine (0-10 μM, 3 min) induces 5-HT release from rat hippocampal synaptosomes by Ca²⁺-dependent way^[2].

体内研究
(In Vivo)

(+)-Norfenfluramine (1-300 μg/kg, i.v.) induces pressor response in conscious SHAM and DOCA-salt rats^[1].
(+)-Norfenfluramine (2.5 and 5 mg/kg, i.p.) decreases of 5-HT and 5-HIAA levels in telencephalon and brainstem of rats^[3].

Animal Model:	Conscious SHAM and DOCA-salt rats^[1].
Dosage:	1-300 μg/kg
Administration:	Intravenous injection (i.v.), given in a cumulative fashion at 6-min intervals.
Result:	Induced pressor response in conscious SHAM and DOCA-salt rats. (change in mean arterial blood pressure at 300 μg/kg, mm Hg, SHAM vehicle=36, SHAM ketanserin=7, DOCA=51, DOCA ketanserin=19).

分子量

203.20

性状

Liquid

Formula

C₁₀H₁₂F₃N

CAS 号

19036-73-8

中文名称

(S)-1-(3-(三氟甲基)苯基)丙-2-胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)