Guanabenz hydrochloride

Product NameGuanabenz hydrochloride
CAS23113-43-1
MFC8H8Cl2N4.ClH
MW267.54
EINECS
MOL File23113-43-1.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	≥4.3 mg/mL in H2O; ≥4.37 mg/mL in EtOH; ≥9.25 mg/mL in DMSO
form	A crystalline solid
color	White to off-white

Usage And Synthesis

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).

Uses

Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure[1][2][3].

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].

in vivo

Guanabenz hydrochloride (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden^[2].
Guanabenz hydrochloride (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice^[2].
Guanabenz hydrochloride (100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min) reduces sympathetic outflow, heart rate and blood pressure in debuffered cats^[3].

Animal Model:	BALB/cJ mice^[2]
Dosage:	5 mg/kg
Administration:	5 mg/kg/day; i.p. ; for 3 weeks
Result:	Reduced the latent brain cysts in both male and female BALB/cJ mice.

Animal Model:	BALB/cJ mice^[2]
Dosage:	5 mg/kg; 10 mg/kg
Administration:	5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks
Result:	Reversed parasite-induced hyperactivity to near-baseline levels.

Animal Model:	Cats^[3]
Dosage:	100 and 320 μg/kg and 1 mg/kg
Administration:	100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min
Result:	Declined markedly blood pressure and nerve activity.

IC 50

Toxoplasma

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.

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