Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H21N7O4S |
| Molecular Weight | 431.469 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(C=C1OC)C(N)=NC(=N2)N3CCN(CC3)C(=O)C4=NN=C(O4)SC
InChI
InChIKey=MULPYFRDYRZMDS-UHFFFAOYSA-N
InChI=1S/C18H21N7O4S/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/h8-9H,4-7H2,1-3H3,(H2,19,20,21)
| 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
| Title | Date | PubMed |
|---|---|---|
| Comparative first dose effects of prazosin and tiodazosin (BL-5111) in spontaneously hypertensive rats. | 1979 Jan |
|
| In vitro comparison of the pre- and postsynaptic alpha adrenergic receptor blocking properties of prazosin and tiodazosin (BL5111). | 1980 |
|
| Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat. | 1980 |
|
| Effect of BL-5111-A, prazosin and phentolamine on responses of canine cutaneous veins to adrenergic activation. | 1980 Apr |
|
| Profile of a new prazosin congener, BL-5111A. Studies in the rat. | 1980 Jan-Feb |
|
| Determination of tiodazosin in plasma and whole blood by high-performance liquid chromatography. | 1982 Jun 11 |
|
| 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
Edited
Fri Dec 15 15:43:29 UTC 2023
by
admin
on
Fri Dec 15 15:43:29 UTC 2023
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| Record UNII |
FQI0PYJ799
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| Record Status |
Validated (UNII)
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| Record Version |
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| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29713
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admin on Fri Dec 15 15:43:29 UTC 2023 , Edited by admin on Fri Dec 15 15:43:29 UTC 2023
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| Code System | Code | Type | Description | ||
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C019578
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Tiodazosin
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4652
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100000077211
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FQI0PYJ799
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66969-81-1
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DTXSID90217180
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CHEMBL2107039
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C72926
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SUB11082MIG
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60891
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
