Details
Stereochemistry | ACHIRAL |
Molecular Formula | 2C9H12Cl2N4O.H2O4S |
Molecular Weight | 624.326 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OS(O)(=O)=O.NC(=N)NNCCOC1=C(Cl)C=CC=C1Cl.NC(=N)NNCCOC2=C(Cl)C=CC=C2Cl
InChI
InChIKey=OLLMPVQGLMNQQK-UHFFFAOYSA-N
InChI=1S/2C9H12Cl2N4O.H2O4S/c2*10-6-2-1-3-7(11)8(6)16-5-4-14-15-9(12)13;1-5(2,3)4/h2*1-3,14H,4-5H2,(H4,12,13,15);(H2,1,2,3,4)
Guanoclor is an anti-hypertensive agent developed by
Pfizer Ltd. (U.K.). It seems to be effective in various types of hypertension
(unknown aetiology, renal, and malignant). It affects both
systolic blood-pressure and diastolic blood-pressure. It is an
adrenergic neurone-blocking agent, which also interferes with
noradrenaline synthesis by inhibition of the enzyme dopamine
beta-hydroxylase. Clinical use of the compound was first
reported by Lawrie et al. (1964), who achieved satisfactory
blood-pressure control in 60% of their cases with guanoclor
alone, and in a further 18% with the addition of a thiazide
diuretic. They also noted a significant reduction in urinary
noradrenaline levels during guanoclor administration. Guanochlor has an affinity for the Na+/H+ exchanger ranging between 0.5 uM and 6 uM in different systems and is more potent than amiloride in all systems studied. It is suggested that guanochlor recognizes a binding site on the Na+/H+ exchanger that is distinct from the amiloride binding site.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14085968
Curator's Comment: Guanoclor induced depletion of noradrenaline in the C.N.S.,
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/5921741
Curator's Comment: The drug has been administered to 35 hypertensive subjects
in doses of from 20 to 240 mg orally each day.
The smallest effective dose used was 20 mg and the
largest 240 mg daily
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3002793
Guanochlor has an affinity for the Na+/H+ exchanger ranging between 0.5 uM and 6 uM in different systems and is more potent than amiloride in all systems studied. Half-maximum inhibition by guanochlor of 45Ca2+ uptake is observed at 30 uM. Half-maximum inhibition of the NaC/H+ exchange system in rabbit renal brush border membrane vesicles is observed at 6 uM guanochlor.
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NCI_THESAURUS |
C270
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Q1U97XK18R
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m223
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DBSALT002915
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SUB14036MIG
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C65834
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21124335
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ACTIVE MOIETY
SUBSTANCE RECORD