Page last updated: 2024-11-04

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 SourceID
PubMed CID1963
CHEMBL ID3246753
CHEBI ID166535
SCHEMBL ID10404543
MeSH IDM0091954

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

ExcerptReferenceRelevance
" 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

ExcerptReferenceRelevance
"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

ExcerptRelevanceReference
" 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)

ClassDescription
triazolobenzodiazepineAny 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 IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1136391Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of nicotine-induced seizures1978Journal 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.
AID1136395Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of maximal electric shock-induced seizures1978Journal 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.
AID1137410Anticonvulsant activity in ip dosed albino CF1 mouse assessed as protection against pentylenetetrazole-induced clonic convulsions1979Journal 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.
AID1136389Effect on motor activity in ip dosed albino CF-1 mouse by dish test1978Journal 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.
AID1137415Reduction of hypoxic stress in ip dosed albino CF1 mouse assessed as prolongation of hypoxic survival time1979Journal 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.
AID1137418Inhibition of oxotremorine-induced hypothermia in ip dosed albino CF1 mouse1979Journal 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.
AID1136390Effect on motor activity in ip dosed albino CF-1 mouse by pedestal test1978Journal 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.
AID1136397Anxiolytic activity in ip dosed albino CF-1 mouse under hypoxic stress1978Journal 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.
AID1137419Potentiation of apomorphine-induced gnawing in ip dosed albino CF1 mouse1979Journal 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.
AID1137412Inhibition of apomorphine-induced cage climbing in ip dosed albino CF1 mouse compound administered prior to challenge measured for 5 mins after 5 mins of challenge1979Journal 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.
AID1136388Effect on motor activity in ip dosed albino CF-1 mouse by chimney test1978Journal 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.
AID1137411Hypothermic activity in ip dosed albino CF1 mouse assessed as effect on body temperature measured after 45 mins1979Journal 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.
AID1136394Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of strychnine-induced seizures1978Journal 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.
AID1136396Antidepressant activity in ip dosed albino CF-1 mouse assessed as inhibition of ethanol-induced response1978Journal 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.
AID1136387Effect on motor activity in ip dosed albino CF-1 mouse by traction test1978Journal 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.
AID1137413Anticonvulsant activity in ip dosed albino CF1 mouse assessed as inhibition of bicucullin-induced tonic extensor convulsions1979Journal 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.
AID1137417Potentiation of yohimbine toxicity in ip dosed aggregated albino CF1 mouse1979Journal 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.
AID1136392Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of pentylenetetrazole-induced seizures1978Journal 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.
AID1137416Inhibition of amphetamine aggregation toxicity in ip dosed albino CF1 mouse compound administered 1 hr prior to challenge measured after 2 hrs1979Journal 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.
AID1137414Antidepressant activity in ip dosed albino CF1 mouse assessed as potentiation of gamma-butyrolactone-induced sleep1979Journal 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.
AID1136393Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of thiosemicarbazide-induced seizures1978Journal 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)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (25.00)18.7374
1990's0 (0.00)18.2507
2000's5 (20.83)29.6817
2010's10 (41.67)24.3611
2020's3 (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.

MetricThis Compound (vs All)
Research Demand Index22.61 (24.57)
Research Supply Index3.43 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (7.14%)5.53%
Reviews0 (0.00%)6.00%
Case Studies4 (14.29%)4.05%
Observational0 (0.00%)0.25%
Other22 (78.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]