150323-78-7

150323-78-7 structure

Name: Quipazine dimaleate
Chemical Name: 2-(1-Piperazinyl)quinoline (2Z)-2-butenedioate (1:2)
CAS Number: 150323-78-7
Molecular Formula: C₂₁H₂₃N₃O₈
Molecular Weight: 445.42300
Catalog: Signaling Pathways Anti-infection SARS-CoV
Create Date: 2018-06-20 12:32:17
Modify Date: 2024-01-08 20:27:10
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].

Name	2-(1-Piperazinyl)quinoline (2Z)-2-butenedioate (1:2)
Synonyms	(+)-Anabasine hydrochloride

Description	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].
Related Catalog	Signaling Pathways >> Anti-infection >> SARS-CoV Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
In Vitro	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: Male and female Wistar rats feed with different sources of the three macronutrients (Group 1: casein, corn starch, safflower oil. Group 2: egg protein, corn starch/sucrose, lard. Group S: casein hydrolysate, maltose dextrin, butter.)[1] Dosage: 2.5, 5 and 7.5 mg/kg Administration: Intraperitoneal injection; 2.5, 5 and 7.5 mg/kg, one dose for once Result: Increased water intake and food intake of male rats from Group S, and reduced food intake of female rats from Group 1 and Group 2s at 2h post-injection. Reduced food intake in female rats from Group 2, reduced protein intake in female rats from Group 1.
References	[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.

Molecular Formula	C₂₁H₂₃N₃O₈
Molecular Weight	445.42300
Exact Mass	445.14900
PSA	177.36000
LogP	1.46180

150323-78-7	64769-66-0
171205-17-7	28614-26-8
22264-50-2	5786-68-5
4774-24-7	1397922-61-0
3978-86-7	850140-73-7