| Bioactivity | 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]. | ||||||||||||
| In Vivo | 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: | ||||||||||||
| Name | Org-12962 | ||||||||||||
| CAS | 132834-56-1 | ||||||||||||
| Formula | C10H11ClF3N3 | ||||||||||||
| Molar Mass | 265.66 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |