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GUANABENZ ACETATE

Basic information Safety Supplier Related

GUANABENZ ACETATE Basic information

Product Name:
GUANABENZ ACETATE
Synonyms:
  • Guanabenz Acetate, ≥98%
  • Guanabenz Acetate - CAS 23256-50-0 - Calbiochem
  • ((2,6-dichlorobenzylidene)amino)-guanidinmonoacetate
  • 2-((2,6-dichlorophenyl)methylene)-hydrazinecarboximidamidmonoacetate
  • br750
  • WY-8678
  • [2,6-DICHLOROBENZYLIDENE)-AMINO]GUANIDINE
  • [(2,6-DICHLOROBENZYLIDENE)AMINO]GUANIDINE ACETATE
CAS:
23256-50-0
MF:
C10H12Cl2N4O2
MW:
291.13
EINECS:
245-534-7
Product Categories:
  • Inhibitors
  • WYTENSIN
Mol File:
23256-50-0.mol
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GUANABENZ ACETATE Chemical Properties

Melting point:
227-229℃ (decomposition)
storage temp. 
Keep in dark place,Inert atmosphere,Room temperature
solubility 
H2O: 11 mg/mL
form 
solid
color 
white
Merck 
14,4558
Stability:
Hygroscopic
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Safety Information

Hazard Codes 
Xn
Risk Statements 
22
Safety Statements 
22-36/37/39-45
RIDADR 
UN 2811 6.1/PG 3
WGK Germany 
3
RTECS 
MF0382000
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
2928002500
Hazardous Substances Data
23256-50-0(Hazardous Substances Data)

MSDS

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GUANABENZ ACETATE Usage And Synthesis

Uses

antihypertensive

Uses

α2-adrenergic agonist and IGRS selective ligand

Definition

ChEBI: Guanabenz acetate is a dichlorobenzene. It has a role as a geroprotector.

brand name

Wytensin (Wyeth).

General Description

Guanabenz acetate, [(2,6-dichlorobenzylidene)amino]guanidine monoacetate (Wytensin), is acentral 2-adrenergic agonist that reduces the release of norepinephrinefrom the neuron when stimulated. The effect ofthe drug results in decreased sympathetic tone in the heart,kidneys, and peripheral blood vessels. The drug does not produceorthostatic hypotension.

Biological Activity

α 2 -adrenergic agonist and IGRS (imidazoline I 2 binding site) selective ligand.

Biochem/physiol Actions

Centrally acting α2 adrenoceptor agonist; I2 imidazoline binding site ligand; antihypertensive.

Pharmacokinetics

The oral bioavailability of guanabenz is 70 to 80%. Following an oral dose, the hypotensive effect of guanabenz begins within 1 hour, peaks within 2 to 7 hours, and is diminished within 6 to 8 hours. It has an elimination half-life averaging 4 to 14 hours. The blood pressure response can persist for at least 12 hours. Following IV dosing, guanabenz is distributed into the CNS, with brain concentrations 3 to 70 times higher than concurrent plasma concentrations. Guanabenz is approximately 90% bound to plasma proteins. In patients with hepatic or renal impairment, its elimination half-life may be prolonged.
Guanabenz is metabolized principally by hydroxylation to its inactive metabolite, 4-hydroxyguanabenz, which is eliminated in the urine as its glucuronide (major) and sulfate conjugates. Guanabenz and its inactive metabolites are excreted principally in urine, with approximately 70 to 80% of its oral dose excreted in urine within 24 hours and approximately 10–30% in feces via enterohepatic cycling. Approximately 40% of an oral dose of guanabenz is excreted in urine as 4-hydroxyguanabenz and its glucuronide, and less than 5% is excreted unchanged. The remainder is excreted as unidentified metabolites and their conjugates.

Clinical Use

Overall, the therapeutic applications for guanabenz are similar to those of clonidine and other α2-adrenergic agonists. One advantage for guanabenz is its once-a-day dosing schedule. Guanabenz has been used in diabetic patients with hypertension without adverse effect on the control of or therapy for diabetes, and it has been effective in hypertensive patients with chronic obstructive pulmonary disease, including asthma, chronic bronchitis, or emphysema. Guanabenz has been used alone or in combination with naltrexone in the management of opiate withdrawal in patients physically dependent on opiates and undergoing detoxification. Guanabenz also has been used as an analgesic in a limited number of patients with chronic pain

Side effects

Overall, the frequency of adverse effects produced by guanabenz is similar to that produced by clonidine and the other α2-adrenergic agonists, but the incidence is lower. As with the other centrally active sympatholytics (e.g., clonidine), abrupt withdrawal of guanabenz may result in rebound hypertension, but the withdrawal syndrome symptoms appear to be less severe.

storage

Store at RT

GUANABENZ ACETATESupplier

Krain Pharmaceutical Technology CO.,Ltd Gold
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18252089365
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Krain_kerun@163.com
J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
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Nanjing Habo Medical Technology Co., Ltd.
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025-85760892 13376090521
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Adamas Reagent, Ltd.
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400-6009262 16621234537
Email
chenyj@titansci.com