Org 12962

Names

[ Name ]:
Org 12962

[Synonym ]:
MFCD00892750

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease

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

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

[Target]

5-HT2C Receptor:7.01 (pEC50)

5-HT2A Receptor:6.38 (pEC50)

5-HT2B Receptor:6.28 (pEC50)

[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: Male Wistar rats[2] Dosage: 0.3 mg/kg, 1 mg/kg, 3.2 mg/kg Administration: Intraperitoneal injection; 0.3-3.2 mg/kg Result: Induced a dose-related antipanic-like effect.

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.454g/cm3

[ Boiling Point ]:
286.004ºC at 760 mmHg

[ Molecular Formula ]:
C₁₀H₁₁ClF₃N₃

[ Molecular Weight ]:
265.66300

[ Flash Point ]:
126.771ºC

[ Exact Mass ]:
265.05900

[ PSA ]:
28.16000

[ LogP ]:
2.55720

[ Vapour Pressure ]:
0.001mmHg at 25°C

[ Index of Refraction ]:
1.541

Safety Information

[ HS Code ]:
2933990090

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%