Page last updated: 2024-12-08

1-hydroxytrimazosin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

It seems you might be referring to **1-hydroxytrimazosin** (also known as **1-HTZ**) rather than 1-hydroxytrimazosin.

**1-HTZ** is a **selective α1-adrenoceptor antagonist** that is structurally similar to trimazosin, a drug used to treat benign prostatic hyperplasia (BPH).

**Why is 1-HTZ important for research?**

* **Mechanism of action:** 1-HTZ is a valuable tool in research because it provides a unique way to study the role of α1-adrenoceptors in various physiological processes. Unlike other α1-adrenoceptor antagonists, 1-HTZ exhibits **selective antagonism for α1A-adrenoceptors** over α1B- and α1D-adrenoceptors. This selectivity allows researchers to investigate the specific functions of α1A-adrenoceptors in different tissues and organs.

* **Potential therapeutic applications:** 1-HTZ's selective antagonism of α1A-adrenoceptors makes it a potential therapeutic agent for various conditions, including:
* **BPH**: α1A-adrenoceptors are heavily involved in smooth muscle contraction of the prostate, so selective blockade of these receptors could offer a targeted approach to treating BPH.
* **Cardiovascular diseases**: 1-HTZ may have potential benefits in conditions like hypertension and heart failure due to its ability to relax vascular smooth muscle.
* **Neurological disorders**: α1A-adrenoceptors play a role in neuronal function, so 1-HTZ could potentially be investigated for its therapeutic potential in conditions like Parkinson's disease and Alzheimer's disease.

* **Research tool for studying α1-adrenoceptor function:** 1-HTZ is used extensively in preclinical research studies to investigate the role of α1A-adrenoceptors in various physiological and pathological processes. This includes:
* **Pharmacological studies**: Determining the affinity and selectivity of 1-HTZ for different α1-adrenoceptor subtypes.
* **In vivo studies**: Investigating the effects of 1-HTZ on blood pressure, smooth muscle function, and other physiological parameters in animal models.
* **Cellular and molecular studies**: Examining the effects of 1-HTZ on α1A-adrenoceptor signaling pathways and downstream targets.

**Overall, 1-HTZ is an important research tool due to its selective antagonism of α1A-adrenoceptors, which provides valuable insights into the role of these receptors in various physiological processes and has potential therapeutic applications in various diseases.**

**It is important to note that 1-HTZ is currently not approved for clinical use and further research is needed to evaluate its safety and efficacy in humans.**

1-hydroxytrimazosin: major metabolite of trimazosin; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID139356
MeSH IDM0120056

Synonyms (11)

Synonym
88321-10-2
2-hydroxy-2-hydroxymethylpropyl-4(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-1-piperazine carboxylic acid
cp 23445
2-hydroxy-2-hydroxymethylpropyl-4(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-1-piperazine caboxylic acid
cp 23,445
cp-23445
1-piperazinecarboxylic acid, 4-(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-, 2,3-dihydroxy-2-methylpropyl ester
1-hydroxytrimazosin
(2,3-dihydroxy-2-methylpropyl) 4-(4-amino-6,7,8-trimethoxyquinazolin-2-yl)piperazine-1-carboxylate
2,3-dihydroxy-2-methylpropyl 4-(4-imino-6,7,8-trimethoxy-3,4-dihydroquinazolin-2-yl)piperazine-1-carboxylate
DTXSID601008059

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters were obtained by computer-assisted, nonlinear, least-squares-fitting regression analysis."( Pharmacokinetics and pharmacodynamics of trimazosin in man.
Elliott, HL; Meredith, PA; Reid, JL, 1983
)
0.27
"3 mg/L), time to peak was strongly delayed by a factor 7, and the time when plasma concentrations were higher than half of Cmax (t Cmax/2) was longer (10."( Pharmacokinetics of a sustained-release trimazosin tablet formulation.
Bianchine, JR; Flouvat, B; Fodor, F; Roux, A, 1983
)
0.27
"The pharmacokinetic and pharmacodynamic profiles of intravenous trimazosin, a postsynaptic alpha 1 antagonist, were analyzed empirically by integrated modelling techniques."( Pharmacokinetic and pharmacodynamic modelling of trimazosin and its major metabolite.
Elliott, HL; Kelman, AW; Meredith, PA; Reid, JL, 1983
)
0.27

Bioavailability

ExcerptReferenceRelevance
" Kinetic analysis showed oral bioavailability of 63%, a clearance rate of 66 ml/min, and a terminal elimination t1/2 of approximately 3 hr."( Trimazosin in normotensive subjects.
Elliott, HL; Hughes, DM; Meredith, PA; Reid, JL; Vincent, J, 1984
)
0.27
" The bioavailability of oral trimazosin was 61 +/- 28%."( Pharmacokinetics and pharmacodynamics of trimazosin in man.
Elliott, HL; Meredith, PA; Reid, JL, 1983
)
0.27
"Pharmacokinetics and bioavailability of a trimazosin sustained-release tablet (SRT) formulation (300 mg) were studied in healthy volunteers."( Pharmacokinetics of a sustained-release trimazosin tablet formulation.
Bianchine, JR; Flouvat, B; Fodor, F; Roux, A, 1983
)
0.27

Dosage Studied

ExcerptRelevanceReference
" This hypotensive effect was maximal between 4 and 6 hr after dosing and was accompanied by a significant increase in heart rate."( Trimazosin in normotensive subjects.
Elliott, HL; Hughes, DM; Meredith, PA; Reid, JL; Vincent, J, 1984
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (100.00)18.7374
1990's0 (0.00)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: 12.25

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.25 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (14.29%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]