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Guanabenz

Guanabenz structure

CAS No:
5051-62-7
Formula:
C8H8Cl2N4
Chemical Name:
Guanabenz
Synonyms:
Hydrazinecarboximidamide,2-[(2,6-dichlorophenyl)methylene]-;Guanidine,[(2,6-dichlorobenzylidene)amino]-;2-[(2,6-Dichlorophenyl)methylene]hydrazinecarboximidamide;N-(2,6-Dichlorobenzylidene)-N′-amidinohydrazine;Guanabenz;[(2,6-Dichlorobenzylidene)amino]guanidine;Wy 8678;NSC 68982
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

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Description

Solid

An alpha-2 selective adrenergic agonist used as an antihypertensive agent.

Guanabenz Basic Attributes

Molecular Weight：

231.08

Exact Mass：

231.08

EC Number：

225-750-8

DSSTox ID：

DTXSID6045666

HScode：

2928000090

Characteristics

PSA：

74.26000

XLogP3：

3.00130

Appearance：

Solid

Density：

1.49g/cm3

Melting Point：

228 °C (decomp)

Boiling Point：

405.7ºC at 760mmHg

Flash Point：

199.1ºC

Refractive Index：

1.645

Water Solubility：

8.89e-02 g/L

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

wgk germany：

hazard class code：

20/21/22-62

safety instructions：

22-36/37/39

Marks：

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P308+P313, P312, P322, P330, P363, P405, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity Summary：

Excessive contraction of the pupils, irritability, low blood pressure, sleepiness, slow heartbeat, sluggishness

Protein Binding：

90%

Drug Information

Drug Indication：

For management of High blood pressure|FDA Label

Pharmacology：

Guanabenz, a centrally acting α-2 adrenergic agonist, is indicated for treatment of hypertension.

MeSH：

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. (See all compounds classified as Adrenergic alpha-2 Receptor Agonists.)|Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

Absorption：

Approximately 75% absorbed from gastrointestinal tract

Metabolism/Metabolites：

Hepatic

Biological Half-Life：

6 hours.

Mechanism of Action：

Guanabenz's antihypertensive effect is thought to be due to central alpha-adrenergic stimulation, which results in a decreased sympathetic outflow to the heart, kidneys, and peripheral vasculature in addition to a decreased systolic and diastolic blood pressure and a slight slowing of pulse rate. Chronic administration of guanabenz also causes a decrease in peripheral vascular resistance.

MeSH Entry Terms：

2,6 Dichlorobenzylideneaminoguanidine

Guanabenz Use and Manufacturing

Uses

alpha agonists

Use Classification：

Human drugs -> Rare disease (orphan)|Pharmaceuticals

Computed Properties

Molecular Weight:231.08
XLogP3:1.7
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:2
Exact Mass:230.0126017
Monoisotopic Mass:230.0126017
Topological Polar Surface Area:76.8
Heavy Atom Count:14
Complexity:228
Undefined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes