| Identification | Back Directory | [Name]
GUANABENZ HYDROCHLORIDE | [CAS]
23113-43-1 | [Synonyms]
NE56490
GUANABENZ HYDROCHLORIDE
Guanabenzhydrochloride(Wytensin)
1-{[(2,6-Dichlorophenyl)methylidene]amino}guanidine Hydrochloride
Hydrazinecarboximidamide, 2-(2,6-dichlorobenzylidene)-, hydrochloride | [Molecular Formula]
C8H9Cl3N4 | [MDL Number]
MFCD01722581 | [MOL File]
23113-43-1.mol | [Molecular Weight]
267.54 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 (Ki = 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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