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Details

Stereochemistry ACHIRAL
Molecular Formula C18H21N7O4S.C5H8O3
Molecular Weight 547.584
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TIODAZOSIN LEVULINATE

SMILES

CC(=O)CCC(O)=O.COC1=CC2=NC(=NC(N)=C2C=C1OC)N3CCN(CC3)C(=O)C4=NN=C(O4)SC

InChI

InChIKey=NIDVOMJMOVCWQI-UHFFFAOYSA-N
InChI=1S/C18H21N7O4S.C5H8O3/c1-27-12-8-10-11(9-13(12)28-2)20-17(21-14(10)19)25-6-4-24(5-7-25)16(26)15-22-23-18(29-15)30-3;1-4(6)2-3-5(7)8/h8-9H,4-7H2,1-3H3,(H2,19,20,21);2-3H2,1H3,(H,7,8)

HIDE SMILES / InChI

Molecular Formula C5H8O3
Molecular Weight 116.1152
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C18H21N7O4S
Molecular Weight 431.469
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Tiodazosin is a newly developed antihypertensive agent, structurally related to prazosin. Prazosin and tiodazosin administrated intravenously to anesthetized rats, are equally effective hypotensive agents, but that the hypotensive potency of prazosin is greater than that of tiodazosin. However, chronic administration of equivalent doses of the two compounds for 25 and 52 days via the drinking water indicated approximately equivalent, sustained reductions in blood pressure. Furthermore, at the end of the 52-day chronic dosing period tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles.

Approval Year

PubMed

PubMed

TitleDatePubMed
The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.
1983 Mar-Apr
Determinations of tiodazosin and levulinic acid from tablets by high-performance liquid chromatography.
1983 Oct
Non-competitive antagonism of the alpha-adrenoceptor-mediated fast component of contraction of rat aorta, by doxazosin and prazosin.
1983 Oct
Effects of tiodazosin, a new antihypertensive, hemodynamics and clinical variables.
1983 Sep
Cardiovascular adrenoreceptor function during compensatory and decompensatory hemorrhagic shock.
1984
[New hypotensive drugs].
1984 Dec 17-31
Determination of tiodazosin concentrations in human plasma with a fluorescence high-performance liquid chromatographic method.
1985 Jul 12
Alteration in the pharmacologic activity of alpha 1 adrenergic antagonists by alpha-1-acid glycoprotein.
1989
The effect of alpha 1-acid glycoprotein on the pharmacological activity of alpha 1-adrenergic antagonists in rabbit aortic strips.
1991 Aug
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:00:01 GMT 2023
Edited
by admin
on Fri Dec 15 15:00:01 GMT 2023
Record UNII
21CC6UVV2J
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TIODAZOSIN LEVULINATE
Common Name English
BR-5111R
Code English
PENTANOIC ACID, 4-OXO-, COMPD. WITH (4-(4-AMINO-6,7-DIMETHOXY-2-QUINAZOLINYL)-1-PIPERAZINYL)(5-(METHYLTHIO)-1,3,4-OXADIAZOL-2-YL)METHANONE (1:1)
Systematic Name English
Code System Code Type Description
PUBCHEM
21312538
Created by admin on Fri Dec 15 15:00:01 GMT 2023 , Edited by admin on Fri Dec 15 15:00:01 GMT 2023
PRIMARY
EPA CompTox
DTXSID20998117
Created by admin on Fri Dec 15 15:00:01 GMT 2023 , Edited by admin on Fri Dec 15 15:00:01 GMT 2023
PRIMARY
FDA UNII
21CC6UVV2J
Created by admin on Fri Dec 15 15:00:01 GMT 2023 , Edited by admin on Fri Dec 15 15:00:01 GMT 2023
PRIMARY
CAS
76798-65-7
Created by admin on Fri Dec 15 15:00:01 GMT 2023 , Edited by admin on Fri Dec 15 15:00:01 GMT 2023
PRIMARY
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ACTIVE MOIETY