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Guanadrel

Guanadrel structure

CAS No:
40580-59-4
Formula:
C10H19N3O2
Chemical Name:
Guanadrel
Synonyms:
Guanidine,N-(1,4-dioxaspiro[4.5]dec-2-ylmethyl)-;Guanidine,(1,4-dioxaspiro[4.5]dec-2-ylmethyl)-;1,4-Dioxaspiro[4.5]decane,guanidine deriv.;N-(1,4-Dioxaspiro[4.5]dec-2-ylmethyl)guanidine;Guanadrel
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

ChEBI: A spiroketal resulting from the formal condensation of the keto group of cyclohexanone with the hydroxy groups of 1-(2,3-dihydroxypropyl)guanidine. A postganglionic adrenergic blocking agent formerly used (generally as the sulfate salt) for the management f hypertension, it has been largely superseded by other drugs less likely to cause orthostatic hypotension (dizzy spells on standing up or stretching).

Solid

Guanadrel is a spiroketal resulting from the formal condensation of the keto group of cyclohexanone with the hydroxy groups of 1-(2,3-dihydroxypropyl)guanidine. A postganglionic adrenergic blocking agent formerly used (generally as the sulfate salt) for the management of hypertension, it has been largely superseded by other drugs less likely to cause orthostatic hypotension (dizzy spells on standing up or stretching). It has a role as an antihypertensive agent and an adrenergic antagonist. It is a member of guanidines and a spiroketal. It is a conjugate base of a guanadrel(1+).|Guanadrel is an antihypertensive agent and postganglionic adrenergic blocking agent.

Guanadrel Basic Attributes

Molecular Weight：

213.281

Exact Mass：

213.28

DSSTox ID：

DTXSID2048533

Characteristics

PSA：

82.9

XLogP3：

0.6

Appearance：

Solid

Density：

1.39g/cm3

Melting Point：

213.5-215 deg C

Boiling Point：

387.9ºC at 760 mmHg

Flash Point：

188.4ºC

Refractive Index：

1.618

Water Solubility：

1.93e+00 g/L

Safety Information

Stability/Shelf Life：

Guanadrel sulfate tablets should be stored in well-closed containers at a temperature less than 40 deg C, preferably between 15-30 deg C.

Toxicity

Toxicity Summary：

Side effects include dizziness, drowsiness, headache, constipation, diarrhea, gas pains, loss of appetite, fatigue, and nasal congestion.

Protein Binding：

Low, approximately 20%

Drug Information

Drug Indication：

Used to treat and control hypertension.

Pharmacology：

High blood pressure adds to the work load of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guanadrel works by controlling nerve impulses along certain nerve pathways. As a result, it relaxes the blood vessels so that blood passes through them more easily. This helps to lower blood pressure.

MeSH：

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：

Rapidly and readily absorbed from the gastrointestinal tract.

Metabolism/Metabolites：

Primarily hepatic

Biological Half-Life：

10 hours

Mechanism of Action：

Guanadrel is an adrenergic neuron inhibitor that slowly displaces norepinephrine from its storage in nerve endings. It blocks the release of norepinephrine in response to the sympathetic nerve stimulation, leading to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position.

MeSH Entry Terms：

guanadrel

Guanadrel Use and Manufacturing

Antihypertensive.

Computed Properties

Molecular Weight:213.28
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:213.147726857
Monoisotopic Mass:213.147726857
Topological Polar Surface Area:82.9
Heavy Atom Count:15
Complexity:245
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Guanadrel

CAS No.: 40580-59-4

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