TIODAZOSIN LEVULINATE

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 Search

SMILES

CC(=O)CCC(O)=O.COC1=CC2=C(C=C1OC)C(N)=NC(=N2)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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6108841 | Elks, J. (2014) The Dictionary of Drugs: Chemical Data, page 1205, retrieved from: https://books.google.ru/books?id=0vXTBwAAQBAJ | Jucker, E. (2013) Progress in Drug Research, page 281, retrieved from: https://books.google.ru/books?id=wFX2BwAAQBAJ

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

Title	Date	PubMed
The effect of alpha 1-acid glycoprotein on the pharmacological activity of alpha 1-adrenergic antagonists in rabbit aortic strips.	1991-08	1681068
Alteration in the pharmacologic activity of alpha 1 adrenergic antagonists by alpha-1-acid glycoprotein.	1989	2571163
Determination of tiodazosin concentrations in human plasma with a fluorescence high-performance liquid chromatographic method.	1985-07-12	4044753
[New hypotensive drugs].	1984-12-17	6097887
Cardiovascular adrenoreceptor function during compensatory and decompensatory hemorrhagic shock.	1984	6323052
Determinations of tiodazosin and levulinic acid from tablets by high-performance liquid chromatography.	1983-10	6644565
Non-competitive antagonism of the alpha-adrenoceptor-mediated fast component of contraction of rat aorta, by doxazosin and prazosin.	1983-10	6140057
Effects of tiodazosin, a new antihypertensive, hemodynamics and clinical variables.	1983-09	6883905
The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.	1983-03-01	6133719
Determination of tiodazosin in plasma and whole blood by high-performance liquid chromatography.	1982-06-11	7107763
Effect of BL-5111-A, prazosin and phentolamine on responses of canine cutaneous veins to adrenergic activation.	1980-04	7406593
Profile of a new prazosin congener, BL-5111A. Studies in the rat.	1980-01-01	7379338
In vitro comparison of the pre- and postsynaptic alpha adrenergic receptor blocking properties of prazosin and tiodazosin (BL5111).	1980	6108842
Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat.	1980	6108841
Comparative first dose effects of prazosin and tiodazosin (BL-5111) in spontaneously hypertensive rats.	1979-01	441514

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:34:39 GMT 2025` Edited by `admin` on `Mon Mar 31 17:34:39 GMT 2025`
Record UNII	21CC6UVV2J
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BR-5111R

Preferred Name

English

TIODAZOSIN LEVULINATE

Common Name

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 Mon Mar 31 17:34:39 GMT 2025 , Edited by admin on Mon Mar 31 17:34:39 GMT 2025

PRIMARY

EPA CompTox

DTXSID20998117

Created by admin on Mon Mar 31 17:34:39 GMT 2025 , Edited by admin on Mon Mar 31 17:34:39 GMT 2025

PRIMARY

FDA UNII

21CC6UVV2J

Created by admin on Mon Mar 31 17:34:39 GMT 2025 , Edited by admin on Mon Mar 31 17:34:39 GMT 2025

PRIMARY

CAS

76798-65-7

Created by admin on Mon Mar 31 17:34:39 GMT 2025 , Edited by admin on Mon Mar 31 17:34:39 GMT 2025

PRIMARY

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