Guanabenz hydrochloride

Description

Guanabenz is an α₂-adrenergic receptor agonist (effective concentrations 10-100 nM) with hypotensive effects. It also competes for imidazoline I₂-binding sites in brown adipose tissue (K_i = 97 nM).

in vitro

maximum concentrations of guanabenz in plasma (1.2 to 5.2 ng/ml) reached 2 to 5 hours after administration of capsules containing 16 or 32 mg of 14c-labelled guanabenz. guanabenz was 90% bound to human plasma proteins [1]. guanabenz competed for imidazoline i2-binding sites in brown adipose tissue with ki of 97 nm [3].

References

[1] holmes b, brogden r n, heel r c, et al. guanabenz[j]. drugs, 1983, 26(3): 212-229.
[2] aantaa r, marjam ki a, scheinin m. molecular pharmacology of α2-adrenoceptor subtypes[j]. annals of medicine, 1995, 27(4): 439-449.
[3] rmer l, wurster s, savola j m, et al. identification and characterization of the imidazoline i2b-binding sites in the hamster brown adipose tissue as a study model for imidazoline receptors[j]. archives of physiology and biochemistry, 2003, 111(2): 159-166.