Quipazine dimaleate

Modify Date: 2024-01-08 20:27:10

Quipazine dimaleate Structure
Quipazine dimaleate structure
Common Name Quipazine dimaleate
CAS Number 150323-78-7 Molecular Weight 445.42300
Density N/A Boiling Point N/A
Molecular Formula C21H23N3O8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Quipazine dimaleate


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].

 Names

Name 2-(1-Piperazinyl)quinoline (2Z)-2-butenedioate (1:2)
Synonym More Synonyms

 Quipazine dimaleate Biological Activity

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
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.  

 Chemical & Physical Properties

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

 Synonyms

(+)-Anabasine hydrochloride