[CAS NO. 132834-56-1] Org-12962
PRODUCTS SPECIFICATIONS [132834-56-1]
DESCRIPTION [132834-56-1]
Overview
| MDL | MFCD00892750 |
|---|---|
| Molecular Weight | 265.66 |
| Molecular Formula | C10H11ClF3N3 |
| SMILES | FC(F)(F)C1=C(N=C(C=C1)N2CCNCC2)Cl |
Summary
Org-12962 is a potent, selective and orally active 5-HT 2C receptor agonist with a pEC 50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT 2A and 5-HT 2B receptor with pEC 50 s of 6.38 and 6.28, respectively [1] [3] .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety [2] .
IC50 & Target
|
5-HT 2C Receptor 7.01 (pEC 50 ) |
5-HT 2A Receptor 6.38 (pEC 50 ) |
5-HT 2B Receptor 6.28 (pEC 50 ) |
In Vivo
Org-12962 (intraperitoneal injection; 0.3-3.2 mg/kg) significantly increases the postinjection frequency thresholds for self-interruption (F
3.71
=11.40). Org-12962 is dissolved or microsuspended in 0.3% v/v Tween 80 in physiological saline (NaCl 0.9%)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 941.05 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.7642 mL | 18.8210 mL | 37.6421 mL |
| 5 mM | 0.7528 mL | 3.7642 mL | 7.5284 mL |
| 10 mM | 0.3764 mL | 1.8821 mL | 3.7642 mL |
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.
