Compounds > tiodazosin
Page last updated: 2024-12-06

tiodazosin

Description

tiodazosin: BL 5111A is for mono-HCl; RN given refers to parent cpd; structure in third source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60891
CHEMBL ID2107039
CHEBI ID177685
SCHEMBL ID121554
MeSH IDM0072131

Synonyms (35)

Synonym
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(5-methylsulanyl-1,3,4-oxadiazol-2-yl)methanone
CHEBI:177685
tiodazosin
tiodazosin (usan/inn)
D06154
66969-81-1
OPREA1_125434
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(5-methylsulfanyl-1,3,4-oxadiazol-2-yl)methanone
CHEMBL2107039
2-(4-((5-methylthio-1,3,4-oxadiazol-2-yl)carbonyl)piperazino)-6,7-dimethoxy-4-chinazolinamin
tiodazosina [inn-spanish]
unii-fqi0pyj799
tiodazosine
bl-5111
tiodazosinum
piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((5-(methylthio)-1,3,4-oxadiazol-2-yl)carbonyl)-
fqi0pyj799 ,
bl 5111
tiodazosin [usan:inn]
tiodazosine [inn-french]
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((5-(methylthio)-1,3,4-oxadiazol-2-yl)carbonyl)-piperazine
tiodazosina
tiodazosinum [inn-latin]
SCHEMBL121554
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[[5-(methylthio)-1,3,4-oxadiazol-2-yl]carbonyl]-piperazine
tiodazosin [usan]
tiodazosin [inn]
MULPYFRDYRZMDS-UHFFFAOYSA-N
4-amino-6,7-dimethoxy-2-[4-(5-methylthio-1,3,4-oxadiazole-2-carbonyl)-piperazin-1-yl]quinazoline
DTXSID90217180
HY-100255
CS-0018406
Q15634026
(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(5-(methylthio)-1,3,4-oxadiazol-2-yl)methanone
AKOS040740402

Research Excerpts

Overview

Tiodazosin (BL5111) is a structural analogue of prazosin. It is currently being evaluated for clinical efficacy in the treatment of hypertension.

ExcerptReferenceRelevance
"Tiodazosin (BL5111) is a structural analogue of prazosin that is currently being evaluated for clinical efficacy in the treatment of hypertension. "( In vitro comparison of the pre- and postsynaptic alpha adrenergic receptor blocking properties of prazosin and tiodazosin (BL5111).
Cohen, ML; Landry, AS; Wiley, KS, 1980)		1.92
"Tiodazosin is a recently developed compound that is currently undergoing investigation for use in hypertension. "( The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.
Baughman, RA; Benet, LZ; Mico, BA, )		1.84

Bioavailability

ExcerptReferenceRelevance
" Lacking an intravenous dosage form for use in human subjects, our study concentrated on the determination of the bioavailability and disposition parameters of tiodazosin in dogs, with a comparison to those parameters for prazosin, obtained from previous work in our laboratory."( The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.
Baughman, RA; Benet, LZ; Mico, BA, )		0.6

Dosage Studied

Tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles.

ExcerptRelevanceReference
" In contrast, BL-5111, an antihypertensive agent similar in chemical structure and shown in previous studies to be slightly less potent than prazosin but with appreciably less alpha-adrenergic receptor antagonist activity, had no effect on blood pressure at 12 hours after dosing (1 and 2 mg/kg po)."( Comparative first dose effects of prazosin and tiodazosin (BL-5111) in spontaneously hypertensive rats.
Buyniski, JP; Florczyk, AP; Roebel, LE, 1979)		0.52
" 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."( Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat.
Buyniski, JP; Campbell, JA; Pircio, AW; Schurig, JE, 1980)		0.89
" Lacking an intravenous dosage form for use in human subjects, our study concentrated on the determination of the bioavailability and disposition parameters of tiodazosin in dogs, with a comparison to those parameters for prazosin, obtained from previous work in our laboratory."( The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.
Baughman, RA; Benet, LZ; Mico, BA, )		0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-arylpiperazine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (88.89)18.7374
1990's1 (11.11)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 98.48

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index98.48 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index173.53 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (98.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		3.5790aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		1.9510naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
wb 4101
N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine bearing a [(2',6'-dimethoxyphenoxy)ethylamino]methyl group at position 2. An alpha1A-adrenergic selective antagonist.		2.3820aromatic ether;
benzodioxine;
secondary amino compound		alpha-adrenergic antagonist
phentolamine
Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.		7.6530imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
phenylephrine
Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.		1.9710phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		3.3470azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
levulinic acid
levulinic acid: inhibits 5-aminolevulinic acid dehydratase; RN given refers to parent cpd; structure in Merck Index, 9th ed, #5316. 4-oxopentanoic acid : An oxopentanoic acid with the oxo group in the 4-position.		6.9610oxopentanoic acid;
straight-chain saturated fatty acid		plant metabolite
trimazosin
trimazosin: RN given refers to parent cpd; structure		6.9510N-arylpiperazine
cocaine
Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.		1.9510benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
ConditionIndicatedRelationship StrengthStudiesTrials
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		01.9610
Blood Pressure, High
[description not available]		02.3620
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		02.3620
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9510
chemdatabank.com