Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H29N5O6 |
Molecular Weight | 435.4742 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(N=C(N=C2N)N3CCN(CC3)C(=O)OCC(C)(C)O)C(OC)=C1OC
InChI
InChIKey=YNZXWQJZEDLQEG-UHFFFAOYSA-N
InChI=1S/C20H29N5O6/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)
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).
Originator
Approval Year
PubMed
Title | Date | PubMed |
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The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade. | 1984 Jan-Feb |
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Pharmacokinetics of trimazosin and its effects on blood pressure, renal function and proteinuria during short-term therapy of patients with impaired renal function and hypertension. | 1986 |
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Activation of the extraneuronal monoamine transporter (EMT) from rat expressed in 293 cells. | 2002 Nov |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7042174
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
Edited
Sun Dec 18 17:32:13 UTC 2022
by
admin
on
Sun Dec 18 17:32:13 UTC 2022
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Record UNII |
31L760807H
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Record Status |
Validated (UNII)
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Record Version |
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-
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Common Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29713
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WHO-VATC |
QC02CA03
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WHO-ATC |
C02CA03
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Code System | Code | Type | Description | ||
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252-732-7
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C75059
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CHEMBL513301
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TRIMAZOSIN
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35795-16-5
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DTXSID50189319
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C005185
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3519
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31L760807H
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M978
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2747
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SUB11298MIG
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DB09206
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37264
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SALT/SOLVATE -> PARENT | |||
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TARGET -> AGONIST | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |