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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
Structure of GUANOCLOR SULFATE

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)

HIDE SMILES / InChI
Molecular Formula C9H12Cl2N4O
Molecular Weight 263.124
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula H2O4S
Molecular Weight 98.078
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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

CNS Active
4002
Curator's Comment: Guanoclor induced depletion of noradrenaline in the C.N.S.,

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Inhibitor
8504
 90.0 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
Vatensol

Approved Use

Unknown
Doses

Doses

DosePopulationAdverse events​
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Disc. AE: Feeling of total lack of energy...
Other AEs: Anginal pain, Feeling of total lack of energy...
AEs leading to
discontinuation/dose reduction:
Feeling of total lack of energy (20%)
Other AEs:
Anginal pain (5%)
Feeling of total lack of energy (25%)
Diarrhoea (5%)
Headache (5%)
Dizziness postural (10%)
Frequency urinary (5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
300 mg 2 times / day multiple, oral
Studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
Disc. AE: Uraemia, Urticaria...
AEs leading to
discontinuation/dose reduction:
Uraemia (2.8%)
Urticaria (2.8%)
Dizziness postural (5.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
AEs

AEs

AESignificanceDosePopulation
Dizziness postural 10%
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Feeling of total lack of energy 20%
Disc. AE
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Feeling of total lack of energy 25%
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Anginal pain 5%
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Diarrhoea 5%
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Frequency urinary 5%
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Headache 5%
600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
https://pubmed.ncbi.nlm.nih.gov/14295356/
Uraemia 2.8%
Disc. AE
300 mg 2 times / day multiple, oral
Studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
Urticaria 2.8%
Disc. AE
300 mg 2 times / day multiple, oral
Studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
Dizziness postural 5.5%
Disc. AE
300 mg 2 times / day multiple, oral
Studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/14085968/
PubMed

PubMed

TitleDatePubMed
Conformational populations for antihistamines and antihypertensives in solution.
1976-04
A comparison of guanoclor and methyldopa in the treatment of severe hypertension.
1971-03
Clinical assessment of the new antihypertensive Compound--1029 (Vatensol)--Guanoclor.
1967-10
Patents

Patents

US6024976
5
US6638528
14
US9016221
15
WO2002045693A1
31

Sample Use Guides

In Vivo Use Guide
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
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.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:06:02 GMT 2025
Edited
by admin
on Mon Mar 31 18:06:02 GMT 2025
Record UNII
Q1U97XK18R
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VATENSOL
Preferred Name English
GUANOCLOR SULFATE
MART.   USAN   WHO-DD  
USAN  
Official Name English
Guanoclor sulfate [WHO-DD]
Common Name English
{[2-(2,6-Dichlorophenoxy)ethyl]amino}guanidine sulfate (2:1)
Systematic Name English
GUANOCLOR SULPHATE
Common Name English
NSC-92354
Code English
GUANOCLOR SULFATE [USAN]
Common Name English
HYDRAZINECARBOXIMIDAMIDE, 2-(2-(2,6-DICHLOROPHENOXY)ETHYL)-, SULFATE (2:1)
Systematic Name English
GUANOCHLOR SULFATE [MI]
Common Name English
GUANOCLOR SULFATE [MART.]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C270
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
Code System Code Type Description
NSC
92354
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
FDA UNII
Q1U97XK18R
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
ECHA (EC/EINECS)
208-996-0
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
ChEMBL
CHEMBL2110641
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
MERCK INDEX
m223
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY Merck Index
DRUG BANK
DBSALT002915
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
EPA CompTox
DTXSID10970467
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
CAS
551-48-4
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
SMS_ID
100000077878
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
EVMPD
SUB14036MIG
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
NCI_THESAURUS
C65834
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
PUBCHEM
21124335
Created by admin on Mon Mar 31 18:06:02 GMT 2025 , Edited by admin on Mon Mar 31 18:06:02 GMT 2025
PRIMARY
Related Record Type Details
Structure of GUANOCLOR
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of GUANOCLOR
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