Quipazine dimaleate_product_DataBase

Bioactivity

Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research[1][2][3][4].

Invitro

Quipazine dimaleate 对 5-HT1 和 5-HT2 具有结合效能，Ki 值均为 230 nM[3]。Quipazine dimaleate 取代大鼠内皮层中 5-HT3R 的 [3H]GR65630，Ki 值为 1.4 nM[3]。Quipazine dimaleate 对大鼠迷走神经具有拮抗作用，对 5-HT2，5-HT1 以及抑制 5-HT 释放的 pIC50 值分别为 6.1，6.49 和 6.17[4]。

In Vivo

Quipazine dimaleate (2.5，5 和 7.5 mg/kg，每个剂量各一次；腹腔注射) 影响雄性和雌性大鼠对不同宏量营养素饮食的膳食自我选择[1]。 Animal Model:

Name

Quipazine dimaleate

CAS

150323-78-7

Formula

C21H23N3O8

Molar Mass

445.42

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Mok E, et al. Effect of quipazine, a selective 5-HT3 agonist, on dietary self-selection of different macronutrient diets in male and female rats. Appetite. 2000 Jun;34(3):313-25. [2]. Günther S, et al. X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease. Science. 2021 May 7;372(6542):642-646. [3]. Glennon RA, et al. 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80. [4]. Ireland SJ, Tyers MB. Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve. Br J Pharmacol. 1987 Jan;90(1):229-38.

PeptideDB

Quipazine dimaleate

CAS: 150323-78-7 F: C21H23N3O8 W: 445.42