Org 12962 HCl

Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model[2].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT2C Receptor:7.01 (pEC50)

5-HT2A Receptor:6.38 (pEC50)

5-HT2B Receptor:6.28 (pEC50)

Org 12962 (intraperitoneal injection; 0.3 mg/kg, 1 mg/kg, and 3.2 mg/kg) displays antiaversive effects in a rat model of panic-like anxiety, it increases the postinjection frequency thresholds for self-interruption (F3.71=11.40). The dose of 0.3 mg/kg ip is not significantly active, that the dose of 1 mg/kg is marginally active and that 3.2 mg/kg ip induced highly significant antiaversive effects[3]. Animal Model: Male Wistar rats[3] Dosage: 0.3 mg/kg, 1 mg/kg, and 3.2 mg/kg Administration: Intraperitoneal injection; 0.3 mg/kg, 1 mg/kg, and 3.2 mg/kg Result: Had a dose-related antipanic-like effect in SD-rat.

[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.