1-hydroxytrimazosin
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 Source | ID |
|---|---|
| PubMed CID | 139356 |
| MeSH ID | M0120056 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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 |
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 6 (100.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (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.
| This Compound (12.25) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (14.29%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (85.71%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||