Org-12962 是选择性，具有口服活性的 5-HT2C 受体激动剂，pEC50 值为 7.01。 Org-12962 对 5-HT2A 和 5-HT2B 受体也具有很高的作用，pEC50 分别为 6.38 和 6.28。Org-12962 在焦虑大鼠的模型中显示出缓解作用。
货号:ajcx15440
CAS:132834-56-1
分子式:C10H11ClF3N3
分子量：265.66
溶解度:DMSO: 250 mg/mL (941.05 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively[1][3].Org-12962 displays antiaversive effects in a rat model of panic-like anxiety[2].

Org-12962 (intraperitoneal injection; 0.3-3.2 mg/kg) significantly increases the postinjection frequency thresholds for self-interruption (F3.71=11.40). Org-12962 is dissolved or microsuspended in 0.3% v/v Tween 80 in physiological saline (NaCl 0.9%)[1]. Animal Model: Male Wistar rats[2]

[1]. Porter RH,et al. Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells.Br J Pharmacol. 1999 Sep;128(1):13-20. [2]. Jenck F, et al. Antiaversive effects of 5HT2C receptor agonists and fluoxetine in a model of panic-like anxiety in rats.Eur Neuropsychopharmacol. 1998 Aug;8(3):161-8. [3]. Faassen F, et al. Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.Int J Pharm. 2003 Sep 16;263(1-2):113-22.