Page last updated: 2024-11-04

meptazinol

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

Description

Meptazinol: A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID41049
CHEMBL ID314437
CHEBI ID91484
SCHEMBL ID25404
MeSH IDM0013440

Synonyms (47)

Synonym
CHEMBL314437
il-22811
BRD-A02710418-003-03-5
AKOS015842890
BPBIO1_001241
einecs 259-109-9
meptazinolum [inn-latin]
3-(3-ethylhexahydro-1-methyl-1h-azepin-3-yl)phenol
brn 1462600
phenol, 3-(3-ethylhexahydro-1-methyl-1h-azepin-3-yl)-
meptazinol [inn:ban]
PRESTWICK2_001004
NCGC00179295-01
BSPBIO_001127
AB00514706
meptazinol
PRESTWICK3_001004
PRESTWICK1_001004
SPBIO_003008
PRESTWICK0_001004
3-(3-ethyl-1-methylazepan-3-yl)phenol
54340-58-8
D08182
meptazinol (inn)
bdbm50373116
unii-18y7s5jkzd
18y7s5jkzd ,
5-21-02-00462 (beilstein handbook reference)
meptazinolum
3-ethyl-hexahydro-3-(3-hydroxyphenyl)-1-methyl-2h-azepine
JLICHNCFTLFZJN-UHFFFAOYSA-N
SCHEMBL25404
HS-0011
meptazinol [who-dd]
meptazinol [inn]
meptazinol [mi]
m-(3-ethylhexahydro-1-methyl-1h-azepin-3-yl)phenol
DTXSID6048543
AB00514706_06
gtpl9083
CHEBI:91484
3-(3-ethyl-1-methyl-3-azepanyl)phenol
Q410618
DB13478
3-(3-ethyl-1-methylhexahydro-1h-azepin-3-yl)phenol
BCP12193
(+/-)-3-(3-ethyl-1-methylhexahydro-1h-azepin-3-yl)phenol

Research Excerpts

Pharmacokinetics

The aim of this paper is to investigate the pharmacokinetic behavior of hydrochloride meptazinol (MEP) in plasma, cerebrospinal fluid (CSF) and cerebral cortex after intranasal administration (8 mg/kg) in male Sprague-Dawley rats.

ExcerptReferenceRelevance
" It is argued that the interaction between these drugs is pharmacokinetic in nature, due probably to an action of ibuprofen on the biotransformation of meptazinol."( Evidence for a pharmacokinetic interaction between ibuprofen and meptazinol in the mouse.
Stephens, RJ, 1984
)
0.27
" Subsequent elimination proceeded in an apparently mono-exponential fashion with a half-life of 2 h, although after intravenous dosage there was evidence of an initial rapid distributive phase."( Pharmacokinetics of the new analgesic, meptazinol, after oral and intravenous administration to volunteers.
Franklin, RA; Graham, DF; Norbury, HM, 1983
)
0.27
"The aim of this paper is to investigate the pharmacokinetic behavior of hydrochloride meptazinol (MEP) in plasma, cerebrospinal fluid (CSF) and cerebral cortex after intranasal administration (8 mg/kg) in male Sprague-Dawley rats."( Pharmacokinetic behavior in plasma, cerebrospinal fluid and cerebral cortex after intranasal administration of hydrochloride meptazinol.
Jiang, X; Shi, Z; Zhang, Q, 2005
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" This method was applied to a pharmacokinetic study of hydrochloride meptazinol tablets in healthy Chinese volunteers."( Liquid chromatography/positive ion electrospray tandem mass spectrometry method for the quantification of hydrochloride meptazinol in human plasma: application to a pharmacokinetic study.
Ge, M; Huang, L; Li, W; Qiao, J; Tan, Z, 2009
)
0.35
" The method proved to be applicable to the pharmacokinetic study of B9M in rat after intravenous and subcutaneous administration."( Determination of Bis(9)-(-)-Meptazinol, a bis-ligand for Alzheimer's disease, in rat plasma by liquid chromatography-tandem mass spectrometry: application to pharmacokinetics study.
Chen, HZ; Ge, XX; Jiang, P; Jiang, T; Qiu, ZB; Rong, ZX; Wang, H; Wang, XL; Xie, Q; Xie, Y; Zhang, QZ, 2012
)
0.38
" The validated method was successfully applied to a preclinical pharmacokinetic study of meserine in mice and rats after intravenous and subcutaneous administration."( Determination of a novel carbamate AChE inhibitor meserine in mouse plasma, brain and rat plasma by LC-MS/MS: application to pharmacokinetic study after intravenous and subcutaneous administration.
Chen, H; Ge, X; Jiang, P; Qiu, Z; Shao, B; Wang, H; Xie, Q; Xie, Y, 2014
)
0.4
"A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for determination of Meserine ((-)-meptazinol phenylcarbamate), a novel potent inhibitor of acetylcholinesterase (AChE), was developed, validated, and applied to a pharmacokinetic study in mice brain."( Determination of Meserine, a new candidate for Alzheimer's disease in mice brain by liquid chromatography-tandem mass spectrometry and its application to a pharmacokinetic and tissue distribution study.
Chen, H; Lv, H; Qiu, Z; Tang, Y; Wang, H; Xie, Q; Xu, J; Zhao, H; Zheng, Z, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
"The respiratory and psychomotor effects of a single oral dose of meptazinol (200 mg) and dextropropoxyphene (65 mg)/paracetamol (650 mg) mixture, was compared alone and in combination with ethanol (0."( Comparison of the effects of therapeutic doses of meptazinol and a dextropropoxyphene/paracetamol mixture alone and in combination with ethanol on ventilatory function and saccadic eye movements.
Ali, NA; Allen, EM; Graham, DF; Marshall, RW; Richens, A, 1985
)
0.27

Bioavailability

compound 3 showed better bioavailability than the parent meptazinol. The prodrug (3) showed a 4-fold increase in oral bioavailability over the parent drugs.

ExcerptReferenceRelevance
" However, the absolute bioavailability of the drug following oral dosage is low (4."( The clinical pharmacokinetics and metabolism of the analgesic meptazinol.
Franklin, RA, 1988
)
0.27
"05) patients than those of the controls (n = 7; 53 +/- 12 ng/ml) reflecting a mean four-fold and two-fold increase in oral bioavailability respectively (cirrhotics: n = 8; 27."( Enhanced oral bioavailability of meptazinol in cirrhosis.
Birnie, GG; Brodie, MJ; Murray, T; Thompson, GG; Watkinson, G, 1987
)
0.27
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" Among these three esters, compound 3 showed better bioavailability than the parent meptazinol."( Synthesis and relative bioavailability of meptazinol benzoyl esters as prodrugs.
Hao, J; Lu, M; Qiu, Z; Zhang, C, 2005
)
0.33
" The prodrug (3) showed a 4-fold increase in oral bioavailability over the parent drug meptazinol in rats."( Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.
Jiang, Z; Qiu, Z; Wang, X; Xie, Q, 2005
)
0.33
" Meserine was rapidly absorbed with a high subcutaneous absolute bioavailability (>90%)."( Determination of a novel carbamate AChE inhibitor meserine in mouse plasma, brain and rat plasma by LC-MS/MS: application to pharmacokinetic study after intravenous and subcutaneous administration.
Chen, H; Ge, X; Jiang, P; Qiu, Z; Shao, B; Wang, H; Xie, Q; Xie, Y, 2014
)
0.4

Dosage Studied

Mephtazinol half-life was somewhat longer than the value of 2 h seen in the young. Peak plasma concentrations after single and multiple dosing were similar for both age groups. There was no significant difference from pretreatment levels either in mean warfarin dosage prothrombin index.

ExcerptRelevanceReference
" After single dosing there were no statistical differences in half-life, clearance, or apparent volume of distribution between the two groups, suggesting that the disposition of meptazinol was not altered by pregnancy."( The disposition of meptazinol after single and multiple intravenous administration to pregnant and non-pregnant women.
Evans, D; Franklin, RA; Graham, DF; Lind, T; Murray, GR, 1989
)
0.28
" Despite substantial intersubject variation in Cmax the plasma concentrations after rectal dosage were higher than after oral administration."( The systemic availability of meptazinol in man after oral and rectal doses.
Franklin, RA; Graham, DF; Jacquot, C; Murray, GR; Petitjean, O; Trouvin, JH, 1989
)
0.28
" A U-shaped dose-response relationship was observed for the ability of CCK-8-S to attenuate (by approximately 50%, at most) morphine-induced tail flick analgesia."( Antagonism of morphine analgesia by CCK-8-S does not extend to all assays nor all opiate analgesics.
Barbaz, BS; Hall, NR; Liebman, JM,
)
0.13
" Self-administered intramuscular analgesia could be instituted by a midwife with a dosage scheme similar to current practice."( Feasibility of self-administration analgesia by the intramuscular route in labour.
Li, DF; Rees, GA; Rosen, M, 1988
)
0.27
"03 mg/kg) paO2 increased and paCO2 decreased, especially after injection of the higher dosage of meptazinol; there was no influence on intrapulmonary right-to-left shunting (Qs/Qt)."( [Meptazinol, a new analgesic. Hemodynamic and respiratory effects].
Boldt, J; Görlach, G; Hempelmann, G; Kling, D; Knoblauch, K; von Bormann, B, 1987
)
0.27
" However, the absolute bioavailability of the drug following oral dosage is low (4."( The clinical pharmacokinetics and metabolism of the analgesic meptazinol.
Franklin, RA, 1988
)
0.27
" However, these changes would not appear to be substantial enough to require a revised dosage recommendation for meptazinol for this age group."( Pharmacokinetics of meptazinol after parenteral administration in the elderly.
Bolland, ME; Franklin, RA; Graham, DF; Lewis, RR; Murray, GR, 1987
)
0.27
" There was no evidence of accumulation after chronic dosing with 200 mg meptazinol four times daily for 13 doses in seven control, seven NCLD and six cirrhotic patients."( Enhanced oral bioavailability of meptazinol in cirrhosis.
Birnie, GG; Brodie, MJ; Murray, T; Thompson, GG; Watkinson, G, 1987
)
0.27
" There was no significant difference from pretreatment levels either in mean warfarin dosage prothrombin index after introduction or withdrawal of meptazinol."( Effect of meptazinol on chronic anticoagulant therapy.
Alm, A; Ryd-Kjellen, E, 1986
)
0.27
" Comparison of these results with those obtained in an earlier study in young volunteers showed that although the half-life of meptazinol was somewhat longer than the value of 2 h seen in the young, peak plasma concentrations after single and multiple dosing were similar for both age groups, implying that clearance remained largely unaltered."( Pharmacokinetics of meptazinol after single and multiple oral administration to elderly patients.
Franklin, RA; Graham, DF; Norbury, HM; Sinha, B, 1984
)
0.27
" A well defined dose-response curve was found for oral meptazinol (50 mg, 100 mg, 150 mg and 200 mg) and placebo."( Tooth pulp stimulation: a method of determining the analgesic efficacy of meptazinol in man.
Gabka, J; Price, RK, 1982
)
0.26
" At the dosage of 1 and 10 mg/kg, meptazinol produced marked anti-nociception and anti-hyperalgesia in non-inflamed and inflamed hindpaw, respectively (P<0."( Antinociceptive effects of meptazinol and its isomers on carrageenan-induced thermal hyperalgesia in rats.
Qiu, ZB; Wang, PF; Zhang, YQ; Zhao, ZQ, 2004
)
0.32
" Furthermore, subcutaneous administration of Bis-Mep (10, 100 or 1000 ng/kg) significantly reversed the scopolamine-induced memory deficits in a typical bell-shaped dose-response manner."( Bis(9)-(-)-nor-meptazinol as a novel dual-binding AChEI potently ameliorates scopolamine-induced cognitive deficits in mice.
Chen, HZ; Cui, Y; Ge, XX; Li, J; Liu, T; Qiu, ZB; Wang, H; Xia, Z; Xie, Q; Xu, J; Xu, JR; Zhang, WW, 2013
)
0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
azepanes
[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]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)18.96000.21005.553710.0000AID1526751
AcetylcholinesteraseMus musculus (house mouse)IC50 (µMol)41.00000.00071.11818.4000AID318846
CholinesteraseMus musculus (house mouse)IC50 (µMol)15.00000.00910.56021.9920AID318847
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1526734Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.05 to 0.5 uM incubated for 2 mins in presence of 2 mM MPP+ by LC-MS/MS analysis relative to control empty vector transfected cells2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID318849Inhibition of human recombinant AChE-induced amyloid beta aggregation at 100 uM by thioflavin T fluorescence method2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID253646Area under curve was determined after intravenous administration (29.7 umol/kg) in rat2005Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.
AID318847Inhibition of mouse serum BChE2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID1526751Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID253647Area under curve was determined after intragastric administration (92.8 umol/kg) in rat2005Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID318848Selectivity for mouse brain AChE over mouse serum BChE2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1526752Passive membrane permeability by LC-MS/MS analysis based PAMPA2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID253573Bioavailability in rat (intragastric administration) (dose 92.8 uM/kg)2005Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1526733Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.5 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID318850Inhibition of human recombinant AChE-induced amyloid beta aggregation at 200 uM by thioflavin T fluorescence method2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID1526731Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.05 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1526732Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.1 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID318846Inhibition of mouse brain AChE2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID318851Inhibition of human recombinant AChE-induced amyloid beta aggregation by thioflavin T fluorescence method2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (191)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990151 (79.06)18.7374
1990's5 (2.62)18.2507
2000's18 (9.42)29.6817
2010's14 (7.33)24.3611
2020's3 (1.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials71 (36.22%)5.53%
Reviews7 (3.57%)6.00%
Case Studies3 (1.53%)4.05%
Observational0 (0.00%)0.25%
Other115 (58.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]