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Details

Stereochemistry ACHIRAL
Molecular Formula C20H29N5O6.ClH
Molecular Weight 471.935
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TRIMAZOSIN HYDROCHLORIDE ANHYDROUS

SMILES

Cl.COC1=CC2=C(N)N=C(N=C2C(OC)=C1OC)N3CCN(CC3)C(=O)OCC(C)(C)O

InChI

InChIKey=KJZWJYNJYOFTNQ-UHFFFAOYSA-N
InChI=1S/C20H29N5O6.ClH/c1-20(2,27)11-31-19(26)25-8-6-24(7-9-25)18-22-14-12(17(21)23-18)10-13(28-3)15(29-4)16(14)30-5;/h10,27H,6-9,11H2,1-5H3,(H2,21,22,23);1H

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C20H29N5O6
Molecular Weight 435.4742
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Trimazosin was originated by Pfizer and was licensed to Bristol-Myers Squibb worldwide except for Canada, Mexico and the USA. Trimazosin is a quinazoline antihypertensive agent structurally related to the selective alpha 1-adrenoceptor blocker prazosin. Trimazosin is an alpha adrenergic receptor antagonist. Compared with prazosin, trimazosin was a less potent but more efficacious hypotensive agent. At doses which caused equal or even greater hypotensive effects than those caused by prazosin, trimazosin caused less inhibition of pressor responses to phenylephrine. When administered during a maximum hypotensive response to prazosin, trimazosin caused an additional fall in pressure. Trimazosin is an effective antihypertensive when given by itself or in combination with a diuretic. Its ability to induce vasodilation without concomitant sodium retention or stimulation of the renin axis may be an important factor in its effectiveness. Trimazosin has the potential to cause sustained improvement in left ventricular function, both at rest and during exercise, in patients with chronic congestive heart failure (CHF).

Approval Year

PubMed

PubMed

TitleDatePubMed
Activation of the extraneuronal monoamine transporter (EMT) from rat expressed in 293 cells.
2002 Nov
Patents

Patents

Sample Use Guides

Trimazosin was given for periods of at least 6 mo to 25 patients with mild to moderate essential hypertension. In doses of 300 to 900 mg dialy trimazosin alone led to blood pressure control (supine diastolic blood pressure less than 90 mm Hg with a fall of at least 10 mm Hg) in 16 patients (64%).
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Fri Dec 15 19:50:59 UTC 2023
Edited
by admin
on Fri Dec 15 19:50:59 UTC 2023
Record UNII
OT29P74170
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TRIMAZOSIN HYDROCHLORIDE ANHYDROUS
Common Name English
1-PIPERAZINECARBOXYLIC ACID, 4-(4-AMINO-6,7,8-TRIMETHOXY-2-QUINAZOLINYL)-, 2-HYDROXY-2-METHYLPROPYL ESTER, HYDROCHLORIDE (1:1)
Common Name English
NSC-355084
Code English
TRIMAZOSIN HYDROCHLORIDE, ANHYDROUS
Common Name English
Code System Code Type Description
CAS
35795-17-6
Created by admin on Fri Dec 15 19:50:59 UTC 2023 , Edited by admin on Fri Dec 15 19:50:59 UTC 2023
PRIMARY
NSC
355084
Created by admin on Fri Dec 15 19:50:59 UTC 2023 , Edited by admin on Fri Dec 15 19:50:59 UTC 2023
PRIMARY
PUBCHEM
64748
Created by admin on Fri Dec 15 19:50:59 UTC 2023 , Edited by admin on Fri Dec 15 19:50:59 UTC 2023
PRIMARY
FDA UNII
OT29P74170
Created by admin on Fri Dec 15 19:50:59 UTC 2023 , Edited by admin on Fri Dec 15 19:50:59 UTC 2023
PRIMARY
ECHA (EC/EINECS)
252-733-2
Created by admin on Fri Dec 15 19:50:59 UTC 2023 , Edited by admin on Fri Dec 15 19:50:59 UTC 2023
PRIMARY
EPA CompTox
DTXSID60189320
Created by admin on Fri Dec 15 19:50:59 UTC 2023 , Edited by admin on Fri Dec 15 19:50:59 UTC 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
SOLVATE->ANHYDROUS
Related Record Type Details
ACTIVE MOIETY