ALEXIS Biochemicals: Fenobam

ALX-550-413

Revised 23-May-06

Fenobam
PRODUCT LINE	Neurobiology
PRODUCT CATEGORY	Glutamate Receptors (Metabotropic) / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-413-M005		5 mg	60.00 USD
ALX-550-413-M025		25 mg	240.00 USD

Product Specification

FORMULA:	C₁₁H₁₁ClN₄O₂
MW:	266.7
CAS NUMBER:	57653-26-6
PURITY:	≥98% (¹H-NMR)
APPEARANCE:	Off-white to pale orange solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
IDENTITY:	Determined by ¹H-NMR and ¹³C-NMR.

Product Description

Potent and selective non-competitive mGluR5 antagonist that displays inverse agonist properties; blocks mGluR5 constitutive activity in vitro (IC₅₀=87nM). Acts at an allosteric modulatory site shared with MPEP (Prod. No. ALX-550-368) and binds mGluR5 with Kd values of 54nM and 31nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo.

Product Specific Literature References

Novel non-benzodiazepine anxiolytics: M.E. Goldberg, et al.; Neuropharmacology 22, 1499 (1983) Abstract
In vitro and in vivo metabolism of the antianxiolytic agent fenobam in the rat: W.N. Wu, et al.; J. Pharm. Sci. 84, 185 (1995) Abstract
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity: R.H. Porter, et al.; J. Pharmacol. Exp. Ther. 315, 711 (2005) Abstract
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues: A. Wallberg et al.; Bioorg. Med. Chem. Lett. 16, 1142 (2006) Abstract