GUANABENZ HYDROCHLORIDE
GUANABENZ HYDROCHLORIDE Basic information
- Product Name:
- GUANABENZ HYDROCHLORIDE
- Synonyms:
-
- GUANABENZ HYDROCHLORIDE
- Hydrazinecarboximidamide, 2-(2,6-dichlorobenzylidene)-, hydrochloride
- 1-{[(2,6-Dichlorophenyl)methylidene]amino}guanidine Hydrochloride
- Guanabenzhydrochloride(Wytensin)
- NE56490
- inhibit,Guanabenz hydrochloride,antiparasitic,Inhibitor,Beta Receptor,Guanabenz,Parasite,Adrenergic Receptor,antihypertensive,high blood pressure
- 2-(2,6-Dichlorobenzylidene)hydrazine-1-carboximidamide hydrochloride
- uanabenz HCl
- CAS:
- 23113-43-1
- MF:
- C8H9Cl3N4
- MW:
- 267.54
- Mol File:
- 23113-43-1.mol
GUANABENZ HYDROCHLORIDE 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
GUANABENZ HYDROCHLORIDE Usage And Synthesis
Description
Guanabenz is an α2-
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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