Page last updated: 2024-12-04
alpha-hydroxytriazolam
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
alpha-hydroxytriazolam: triazolam metabolite; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 1963 |
CHEMBL ID | 3246753 |
CHEBI ID | 166535 |
SCHEMBL ID | 10404543 |
MeSH ID | M0091954 |
Synonyms (28)
Synonym |
---|
4h-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine-1-methanol, 8-chloro-6-(2-chlorophenyl)- |
37115-45-0 |
CHEBI:166535 |
[8-chloro-6-(2-chlorophenyl)-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-1-yl]methanol |
alpha-hydroxytriazolam |
j53y2m2sah , |
unii-j53y2m2sah |
1-hydroxymethyltriazolam |
1'-hydroxy triazolam |
CHEMBL3246753 |
6-(o-chlorophenyl)-8-chloro-4h-s-triazolo[4,3-a][1,4]benzodiazepine-1-methanol |
8-chloro-6-(o-chlorophenyl)-1-hydroxymethyl-4h-s-triazolo[4,3-a] [1,4]benzodiazepine |
6-(o-chlorophenyl)-8-chloro-4 h-s-triazolo[4,3-a] [1,4]benzodiazepine-1-methanol |
8-chloro-1-(hydroxymethyl)-6-(o-chlorophenyl)-4h-s-triazolo[4,3-a][1,4]benzodiazepine |
.alpha.-hydroxy-triazolam |
SCHEMBL10404543 |
AKOS030254397 |
alpha-hydroxytriazolam 0.1 mg/ml in methanol |
alpha-hydroxytriazolam 1.0 mg/ml in methanol |
NCGC00485016-01 |
1'-hydroxytriazolam |
(e)-(8-chloro-6-(2-chlorophenyl)-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-1-yl)methanol |
2-(4-chloro-2-nitriphenyl)aminobenzoicacid |
.alpha.-hydroxytriazolam |
8-chloro-6-(o-chlorophenyl)-4h-s-triazolo(4,3-a)(1,4)benzodiazepin-1-methanol |
alpha-hydroxytriazolam solution |
DTXSID50958284 |
alpha-hydroxytriazolam, 1mg/ml in methanol |
Research Excerpts
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
" There were no changes in the half-life of triazolam or alpha-hydroxytriazolam." | ( Effect of ranitidine on the pharmacokinetics of triazolam and alpha-hydroxytriazolam in both young (19-60 years) and older (61-78 years) people. Kersey, K; Koch, KM; Lam, R; O'Connor-Semmes, RL; Williams, DH, 2001) | 0.8 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Dosage Studied
Excerpt | Relevance | Reference |
---|---|---|
" The study provides further evidence of the lack of change in pharmacokinetic parameters on multiple dosing and that drug accumulation did not occur." | ( Pharmacokinetics of triazolam in geriatric patients. Abrahamsson, L; Björnson, G; Börjesson, L; Dehlin, O; Smith, RB, 1983) | 0.27 |
"25 mg (1) alone, (2) on the third day of dosing ranitidine 75 mg twice daily for 4 days, and (3) on the third day of dosing ranitidine 150 mg twice daily for 4 days." | ( Effect of ranitidine on the pharmacokinetics of triazolam and alpha-hydroxytriazolam in both young (19-60 years) and older (61-78 years) people. Kersey, K; Koch, KM; Lam, R; O'Connor-Semmes, RL; Williams, DH, 2001) | 0.55 |
" Eighteen guinea pigs were divided into three dosage groups (10, 100, and 500 microg/kg) and administrated a single dose of triazolam intragastrically." | ( Determination of triazolam and alpha-hydroxytriazolam in guinea pig hair after a single dose. Shen, B; Shen, M; Sun, Q; Xiang, P; Yan, H, 2010) | 0.65 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
Class | Description |
---|---|
triazolobenzodiazepine | Any organic heterotricyclic compound that is any benzodiazepine which is ortho-fused with a triazole. |
[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] |
Bioassays (26)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1136391 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of nicotine-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1136395 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of maximal electric shock-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1137410 | Anticonvulsant activity in ip dosed albino CF1 mouse assessed as protection against pentylenetetrazole-induced clonic convulsions | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1136389 | Effect on motor activity in ip dosed albino CF-1 mouse by dish test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1137415 | Reduction of hypoxic stress in ip dosed albino CF1 mouse assessed as prolongation of hypoxic survival time | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1137418 | Inhibition of oxotremorine-induced hypothermia in ip dosed albino CF1 mouse | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1136390 | Effect on motor activity in ip dosed albino CF-1 mouse by pedestal test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1136397 | Anxiolytic activity in ip dosed albino CF-1 mouse under hypoxic stress | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1137419 | Potentiation of apomorphine-induced gnawing in ip dosed albino CF1 mouse | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1137412 | Inhibition of apomorphine-induced cage climbing in ip dosed albino CF1 mouse compound administered prior to challenge measured for 5 mins after 5 mins of challenge | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1136388 | Effect on motor activity in ip dosed albino CF-1 mouse by chimney test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1137411 | Hypothermic activity in ip dosed albino CF1 mouse assessed as effect on body temperature measured after 45 mins | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1136394 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of strychnine-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1136396 | Antidepressant activity in ip dosed albino CF-1 mouse assessed as inhibition of ethanol-induced response | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1136387 | Effect on motor activity in ip dosed albino CF-1 mouse by traction test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1137413 | Anticonvulsant activity in ip dosed albino CF1 mouse assessed as inhibition of bicucullin-induced tonic extensor convulsions | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1137417 | Potentiation of yohimbine toxicity in ip dosed aggregated albino CF1 mouse | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1136392 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of pentylenetetrazole-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
AID1137416 | Inhibition of amphetamine aggregation toxicity in ip dosed albino CF1 mouse compound administered 1 hr prior to challenge measured after 2 hrs | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1137414 | Antidepressant activity in ip dosed albino CF1 mouse assessed as potentiation of gamma-butyrolactone-induced sleep | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
AID1136393 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of thiosemicarbazide-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (24)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 6 (25.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 5 (20.83) | 29.6817 |
2010's | 10 (41.67) | 24.3611 |
2020's | 3 (12.50) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 22.61
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (22.61) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 2 (7.14%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 4 (14.29%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 22 (78.57%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |