| Bioactivity | Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research[1][2][3][4]. |
| Invitro | Quipazine 对 5-HT1 和 5-HT2 具有结合效能,Ki 值均为 230 nM[3]。Quipazine 取代大鼠内皮层中 5-HT3R 的 [3H]GR65630,Ki 值为 1.4 nM[3]。Quipazine 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 (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]。 |
| Name | Quipazine |
| CAS | 4774-24-7 |
| Formula | C13H15N3 |
| Molar Mass | 213.28 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 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. |