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allylamine

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Description

Allylamine: Possesses an unusual and selective cytotoxicity for VASCULAR SMOOTH MUSCLE cells in dogs and rats. Useful for experiments dealing with arterial injury, myocardial fibrosis or cardiac decompensation. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID7853
CHEMBL ID57286
CHEBI ID188938
MeSH IDM0000751

Synonyms (65)

Synonym
allyl-amine
nsc-7600
107-11-9
wln: z2u1
allylamine
2-propen-1-amine
3-aminopropylene
nsc7600
2-propenylamine
2-propenamine
3-amino-1-propene
3-aminopropene
monoallylamine
inchi=1/c3h7n/c1-2-3-4/h2h,1,3-4h
prop-2-en-1-amine
hsdb 2065
ccris 4746
un2334
ai3-23214
nsc 7600
einecs 203-463-9
brn 0635703
NCGC00159381-02
allylamine, 98%
allylamine, >=99%
3 aminopropylene
CHEMBL57286
CHEBI:188938
AKOS000119634
4-04-00-01057 (beilstein handbook reference)
unii-48g762t011
48g762t011 ,
ec 203-463-9
allylamine [un2334] [poison]
A0219
allyl amine
30551-89-4
allylamine [hsdb]
allylamine [mi]
2-propen-1-ylamine
allylaminehydrochloride
(2-propenyl)amine
2-propenyl amine
1-amino-2-propene
allylamin
ailylamine
n-allylarnine
n-allylamine
un 2334
ch2=chch2nh2
DTXSID8024440 ,
mfcd00008199
F2190-0363
allylamine, puriss., >=99.5% (gc)
allylamine, purum, >=98.0% (gc)
allylamine;3-amino-1-propene
Q417414
BCP27099
bdbm50225454
STL185583
STR00193
EN300-19995
2-propene-1-amine
dtxcid404440
1-aminoprop-2-ene

Research Excerpts

Overview

Allylamine (AA) is an electrophilic amine with a long history of experimental usage because of its extremely potent and relatively specific cardiovascular toxicity. The allylamine derivatives are a new class of synthetic antifungal agents.

ExcerptReferenceRelevance
"Allylamine (AA) is an electrophilic amine with a long history of experimental usage because of its extremely potent and relatively specific cardiovascular toxicity; it has been utilized in a variety of experimental models attempting to mimic human atherosclerotic lesions, myocardial infarction, and vascular injury. "( Glutathione S-transferase 8-8 is localized in smooth muscle cells of rat aorta and is induced in an experimental model of atherosclerosis.
Awasthi, S; Awasthi, YC; Boor, PJ; Misra, P; Singhal, SS; Srivastava, SK, 1995
)
1.73
"The allylamine derivatives are a new class of synthetic antifungal agents. "( Antidermatophytic activity of allylamine derivatives.
Venugopal, PV; Venugopal, TV, 1994
)
1.14
"Allylamines are a new class of antimycotic compounds with a new mechanism of antifungal action, i.e., inhibition of the fungal squalene epoxidase."( Effects of naftifine and terbinafine, two allylamine antifungal drugs, on selected functions of human polymorphonuclear leukocytes.
Baldi, G; Barbareschi, M; Bevilacqua, M; Colombo, D; Dallegri, F; Norbiato, G; Vago, T, 1994
)
1.27
"Allylamines are a newly developed group of drugs possessing a broad spectrum of activity against a wide range of fungi. "( Disk diffusion susceptibility testing of dermatophytes with allylamines.
Venugopal, PV; Venugopal, TV, 1994
)
1.97
"Allylamine is an aliphatic amine that causes vascular lesions in aorta and medium-sized arteries. "( Lipid peroxidation and oxidative stress during acute allylamine-induced cardiovascular toxicity.
Awasthi, S; Boor, PJ,
)
1.82
"Allylamine is a specific cardiovascular toxin that causes vascular and myocardial lesions. "( Semicarbazide protection from in vivo oxidant injury of vascular tissue by allylamine.
Awasthi, S; Boor, PJ, 1993
)
1.96
"Allylamine (AA) is a cardiovascular toxin that causes lesions resembling atherosclerosis in several mammalian species. "( Role of glutathione S-transferase 8-8 in allylamine resistance of vascular smooth muscle cells in vitro.
Awasthi, S; Boor, PJ; He, N; Singhal, SS; Zhao, T, 1999
)
2.01
"The allylamines are a new class of antifungal drugs that inhibit ergosterol synthesis at the level of squalene epoxidase. "( Pharmacology of the allylamines.
Birnbaum, JE, 1990
)
1.16

Effects

Allylamine has been shown to bind to mitochondria from aorta and heart. This suggests that the subcellular site of injury is at or near the mitochondrion.

ExcerptReferenceRelevance
"Allylamine has been shown to bind to mitochondria from aorta and heart, suggesting that the subcellular site of injury is at or near the mitochondrion."( Inhibition of rat heart mitochondrial electron transport in vitro: implications for the cardiotoxic action of allylamine or its primary metabolite, acrolein.
Biagini, RE; Lynch, DW; Toraason, MA; Winston, GW, 1990
)
1.21
"Allylamine has been given by a variety of routes to many species in attempts to cause lesions which mimic human acute vasculitis, acute myocardial necrosis, and atherosclerosis; examples of typical lesions are illustrated."( Allylamine cardiovascular toxicity.
Boor, PJ; Hysmith, RM, 1987
)
2.44

Treatment

Treatment with allylamine resulted in subendocardial fibrosis (size = 4.2%) in 4 of 12 rats. The vasomotor response to LDV, but not RGD, was attenuated in a dose-dependent manner.

ExcerptReferenceRelevance
"In allylamine-treated rats (AAM), the vasomotor response to LDV, but not RGD, was attenuated in a dose-dependent manner."( Modulation of alpha4 integrin mRNA levels is coupled to deficits in vasomotor function in rat arterioles by allylamine.
Chao, JT; Crow, TY; Meininger, GA; Neiger, JD; Partridge, CR; Ramos, KS; Williams, ES; Wilson, E, 2005
)
1.06
"Treatment with allylamine resulted in subendocardial fibrosis (size = 4.2%) in 4 of 12 rats."( Ethanol ingestion on allylamine-induced experimental subendocardial fibrosis.
Imai, S; Izumi, T; Kato, K; Masani, F; Nakazawa, M; Shibata, A,
)
0.79

Toxicity

Allylamine (AA) and beta-aminopropionitrile (beta APN) are well known vascular toxins with a demonstrated synergistic toxic effect. Acrolein may cause allylamine's toxic effects, since it acts as a strong peroxidizing agent.

ExcerptReferenceRelevance
"The underlying etiology of the toxic oil syndrome may be related to any of several toxic contaminants."( Synergistic vascular toxicity and fatty acid anilides in the toxic oil syndrome.
Ansari, GA; Boor, PJ; Jerrells, TR; Kaphalia, BS; Khan, MF, 1991
)
0.28
" Allylamine's toxic effect on myocardium in this model may be mediated through its metabolism and subsequent injurious intracellular events."( Allylamine and acrolein toxicity in perfused rat hearts.
Anderson, PG; Boor, PJ; Sklar, JL, 1991
)
2.63
"Allylamine is toxic to the cardiovascular system causing aortic, valvular and myocardial lesions."( Comparative toxicity of allylamine and acrolein in cultured myocytes and fibroblasts from neonatal rat heart.
Biagini, RE; Breitenstein, M; Krueger, JA; Luken, ME; Toraason, M, 1989
)
2.03
" These results support the concept that AAM is oxidatively deaminated by an SSAO present in vascular cells to generate toxic metabolic by-products capable of causing extensive cellular injury."( Allylamine-induced vascular toxicity in vitro: prevention by semicarbazide-sensitive amine oxidase inhibitors.
Cox, LR; Grossman, SL; Ramos, K, 1988
)
1.72
" The general toxic effects of the freebase form are primarily related to irritation of the mucous membranes, whereas the relatively long history of experimental use of this chemical has emphasized its' extraordinarily deleterious effects on heart and vascular tissue."( Allylamine cardiovascular toxicity.
Boor, PJ; Hysmith, RM, 1987
)
1.72
"This study supports a recent hypothesis that the cardiovascular toxin, allylamine, is toxic to smooth muscle cells of large elastic arteries (aorta)."( Comparative toxicity of the cardiovascular toxin allylamine to porcine aortic smooth muscle and endothelial cells.
Boor, PJ; Hysmith, RM, 1986
)
0.76
" Acrolein may cause allylamine's toxic effects, since it acts as a strong peroxidizing agent itself; in addition, deamination of allylamine is accompanied by production of hydrogen peroxide."( Lipid peroxidation and oxidative stress during acute allylamine-induced cardiovascular toxicity.
Awasthi, S; Boor, PJ,
)
0.7
" Adverse effects were minimal and included mild peeling in two patients and mild fissuring with transient fingertip numbness in one patient."( Open-label study of the safety and efficacy of naftifine hydrochloride 1 percent gel in patients with distal subungual onychomycosis of the fingers.
Cohen, JL; Hochman, LG; Holwell, JE; Meyerson, MS; Pappert, AS; Scher, RK, 1993
)
0.29
"The ability of allylamine (AA) administration to produce vascular lesions resembling atherosclerotic disease in animals, has been linked to metabolism of AA to the toxic aldehyde acrolein (ACR) by a semicarbazide-sensitive amine oxidase (SSAO) found in plasma and in vascular smooth muscle."( [Effect of activity of semicarbazide-sensitive aminooxidases and cellular glutathione on the cytotoxic effect of allylamine, acrolein, and formaldehyde in human cultured endothelial cells].
Lyles, GA; Pino, R,
)
0.7
" Our data show that AA and its aldehyde metabolite, acrolein, were the most toxic compounds to both cell types."( Contribution of serum and cellular semicarbazide-sensitive amine oxidase to amine metabolism and cardiovascular toxicity.
Boor, PJ; Conklin, DJ; Langford, SD, 1998
)
0.3
"To compare colesevelam hydrochloride (Cholestagel), a nonabsorbed hydrogel with bile acid-sequestering properties, with placebo for its lipid-lowering efficacy, its effects on laboratory and clinical safety parameters, and the incidence of adverse events."( Colesevelam hydrochloride (cholestagel): a new, potent bile acid sequestrant associated with a low incidence of gastrointestinal side effects.
Burke, SK; Davidson, MH; Dillon, MA; Gordon, B; Isaacsohn, J; Jones, P; Samuels, J; Toth, P; Weiss, S, 1999
)
0.3
" Patients returned to the clinic every 2 weeks throughout the treatment period for lipid parameter measurements and adverse event assessments."( Colesevelam hydrochloride (cholestagel): a new, potent bile acid sequestrant associated with a low incidence of gastrointestinal side effects.
Burke, SK; Davidson, MH; Dillon, MA; Gordon, B; Isaacsohn, J; Jones, P; Samuels, J; Toth, P; Weiss, S, 1999
)
0.3
" The incidence of adverse events was similar among all groups."( Colesevelam hydrochloride (cholestagel): a new, potent bile acid sequestrant associated with a low incidence of gastrointestinal side effects.
Burke, SK; Davidson, MH; Dillon, MA; Gordon, B; Isaacsohn, J; Jones, P; Samuels, J; Toth, P; Weiss, S, 1999
)
0.3
" Interest lies in estimating relevant doses among those under investigation for efficacy and safety variables, such as the minimum effective dose or the maximum safe dose (or estimating both doses simultaneously)."( Identifying effective and/or safe doses by stepwise confidence intervals for ratios.
Bretz, F; Hothorn, LA; Hsu, JC, 2003
)
0.32
"WelChol (colesevelam hydrochloride), a bile acid sequestrant for the treatment of hypercholesterolemia, was evaluated for adverse effects on reproduction and fetal development using standard preclinical tests."( Colesevelam hydrochloride does not cause maternal or fetal toxicity in rats and rabbits.
Baker, BA; Dagher, R; Jones, MR; Marquis, JK, 2006
)
0.33
" Both treatment regimens were safe and well tolerated."( Safety and efficacy of colesevelam hydrochloride in combination with fenofibrate for the treatment of mixed hyperlipidemia.
Abby, S; Jones, M; McKenney, J, 2005
)
0.33
" Of recipients of colesevelam and placebo, respectively, 30 and 26 discontinued the study prematurely; 7 and 9 withdrew because of protocol-specified hyperglycemia, and 10 and 4 withdrew because of adverse events."( Efficacy and safety of colesevelam in patients with type 2 diabetes mellitus and inadequate glycemic control receiving insulin-based therapy.
Fonseca, VA; Goldberg, RB; Jones, MR; Truitt, KE, 2008
)
0.35
"Colesevelam treatment seems to be safe and effective for improving glycemic control and lipid management in patients with type 2 diabetes mellitus receiving insulin-based therapy, and it may provide a novel treatment for improving dual cardiovascular risk factors."( Efficacy and safety of colesevelam in patients with type 2 diabetes mellitus and inadequate glycemic control receiving insulin-based therapy.
Fonseca, VA; Goldberg, RB; Jones, MR; Truitt, KE, 2008
)
0.35
" Safety and tolerability of colesevelam hydrochloride was evaluated by the incidence and severity of adverse events."( Long-term Safety and Tolerability of Colesevelam HCl in Subjects with Type 2 Diabetes.
Fonseca, VA; Ford, DM; Goldfine, AB; Jones, MR; Truitt, KE; Wang, AC, 2010
)
0.36
" Adverse events were also evaluated."( Colesevelam hydrochloride: efficacy and safety in pediatric subjects with heterozygous familial hypercholesterolemia.
Hopkins, PN; Karki, S; Marais, AD; Melino, M; Misir, S; Raal, FJ; Schurr, D; Stein, EA; Szamosi, T; Urbina, EM; Xu, J, 2010
)
0.36
" Drug-related adverse events were reported by 36."( A 50-week extension study on the safety and efficacy of colesevelam in adults with primary hypercholesterolemia.
Davidson, MH; Donovan, JM; Jones, MR; Misir, S, 2010
)
0.36
"In this study, colesevelam was found to be safe and effective for the management of LDL-C levels in adults with primary hypercholesterolemia."( A 50-week extension study on the safety and efficacy of colesevelam in adults with primary hypercholesterolemia.
Davidson, MH; Donovan, JM; Jones, MR; Misir, S, 2010
)
0.36
" Safety was assessed by adverse events and changes from baseline in clinical status and laboratory studies."( A double-blind, randomized, vehicle-controlled study evaluating the efficacy and safety of naftifine 2% cream in tinea cruris.
Avakian, E; Fleischer, AB; Hardas, B; Olayinka, B; Pappert, EJ; Parish, JL; Parish, LC; Plaum, S; Routh, HB, 2011
)
0.37
" Safety was evaluated by adverse events (AE) and laboratory values in 707 subjects."( A randomized, double-blind, vehicle-controlled efficacy and safety study of naftifine 2% cream in the treatment of tinea pedis.
Avakian, EV; Fleischer, AB; Hardas, B; Parish, JL; Parish, LC; Plaum, S; Routh, HB, 2011
)
0.37
"Topical NAFT-2 for two weeks is safe and provides significantly superior antifungal treatment than vehicle in tinea pedis subjects."( A randomized, double-blind, vehicle-controlled efficacy and safety study of naftifine 2% cream in the treatment of tinea pedis.
Avakian, EV; Fleischer, AB; Hardas, B; Parish, JL; Parish, LC; Plaum, S; Routh, HB, 2011
)
0.37
" Safety was evaluated by adverse events (AE) and laboratory values in 1714 subjects (n=1143, naftifine; n=571, vehicle)."( Efficacy and safety of naftifine HCl Gel 2% in the treatment of interdigital and moccasin type tinea pedis: pooled results from two multicenter, randomized, double-blind, vehicle-controlled trials.
Fleischer, AB; Hardas, B; Kircik, L; Olayinka, B; Parish, LC; Plaum, S; Stein Gold, LF; Verma, A; Vlahovic, T, 2013
)
0.39
" Treatment related adverse events were minimal."( Efficacy and safety of naftifine HCl Gel 2% in the treatment of interdigital and moccasin type tinea pedis: pooled results from two multicenter, randomized, double-blind, vehicle-controlled trials.
Fleischer, AB; Hardas, B; Kircik, L; Olayinka, B; Parish, LC; Plaum, S; Stein Gold, LF; Verma, A; Vlahovic, T, 2013
)
0.39
" Low-density lipoprotein cholesterol (LDL-C), A1C, and adverse events were assessed."( Safety and efficacy of colesevelam HCl in the treatment of elderly patients.
Ford, DM; Gavin, JR; Jones, MR; Truitt, KE, 2014
)
0.4
" In both analyses, adverse event incidence was generally similar between subgroups."( Safety and efficacy of colesevelam HCl in the treatment of elderly patients.
Ford, DM; Gavin, JR; Jones, MR; Truitt, KE, 2014
)
0.4
" There were no serious drug-related adverse events, and the majority of adverse events were mild or moderate."( Efficacy and safety of colesevelam in combination with pioglitazone in patients with type 2 diabetes mellitus.
Baz-Hecht, M; Chou, HS; Ford, DM; Rosenstock, J; Tao, B; Truitt, KE, 2014
)
0.4
" Safety was evaluated by adverse events (AE) and laboratory values in 231 subjects (n=116, naftifine; n=115, vehicle)."( Efficacy and Safety of Naftifine HCl Cream 2% in the Treatment of Pediatric Subjects With Tinea Corporis.
Dhawan, S; Dobrowski, D; Gold, M; Kuligowski, M; Verma, A, 2016
)
0.43
" Treatment related adverse events were minimal."( Efficacy and Safety of Naftifine HCl Cream 2% in the Treatment of Pediatric Subjects With Tinea Corporis.
Dhawan, S; Dobrowski, D; Gold, M; Kuligowski, M; Verma, A, 2016
)
0.43
" Complete cure, growth inhibition, or adverse events served as outcomes."( Safety and efficacy of allylamines in the treatment of cutaneous and mucocutaneous leishmaniasis: A systematic review.
Bezemer, JM; de Vries, HJC; Limpens, J; Schallig, HDFH; van der Ende, J, 2021
)
0.93

Pharmacokinetics

ExcerptReferenceRelevance
" The mean plasma half-life of elimination (t1/2 beta) was about the same following oral (2."( Clinical pharmacokinetics and oral bioavailability of ketobemidone.
Anderson, P; Arnér, S; Bondesson, U; Boréus, LO; Hartvig, P, 1980
)
0.26
"The pharmacokinetic constants and rectal bioavailability of the narcotic analgesic ketobemidone were determined in six male patients after surgery."( Clinical pharmacokinetics of ketobemidone. Its bioavailability after rectal administration.
Anderson, P; Arnér, S; Bondesson, U; Boréus, LO; Hartvig, P, 1981
)
0.26
" A split-dosing regimen resulted in alterations in pharmacokinetic parameters for lovastatin and lovastatin hydroxyacid that are likely due to known differences in the pharmacokinetics of lovastatin when administered to patients with meals or in a fasting state."( Effect of colesevelam on lovastatin pharmacokinetics.
Burke, SK; Donovan, JM; Kisicki, JC; Stiles, MR; Tracewell, WG, 2002
)
0.31
" For the colesevelam coadministration periods, 3,750 mg once daily was dosed throughout the pharmacokinetic sampling period."( The effects of colesevelam HCl on the single-dose pharmacokinetics of glimepiride, extended-release glipizide, and olmesartan medoxomil.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014
)
0.4
" Colesevelam (3750mg once daily) was dosed throughout the pharmacokinetic sampling period."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014
)
0.4
"For all six test drugs, 90% CIs for geometric least-squares mean ratios of AUC and Cmax for the measured analytes were within specified limits, indicating no interaction between the test drug and colesevelam."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014
)
0.4
" Although the phenytoin study indicated no pharmacokinetic interaction, phenytoin should continue to be taken ≥4h before colesevelam in accordance with current prescribing information."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014
)
0.4
" Pharmacokinetic blood and urine samples were collected at various time points throughout the study."( An Open-Label, Multi-Center, Multiple-Application Pharmacokinetic Study of Naftifine HCl Gel 2% in Pediatric Subjects With Tinea Pedis.
Fleischer, AB; Olayinka, B; Verma, A, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
"The primary aim of this study was to compare the effect of colesevelam HCl in combination with ezetimibe to ezetimibe monotherapy on low-density lipoprotein cholesterol (LDL-C) levels in subjects with primary hypercholesterolemia."( Lipid-lowering effects of colesevelam HCl in combination with ezetimibe.
Abby, S; Bays, H; Jones, M; Lai, YL; Rhyne, J, 2006
)
0.33

Bioavailability

ExcerptReferenceRelevance
" When given orally, terbinafine is well absorbed and rapidly and extensively distributed to the skin and sebum in concentrations that exceed the minimum inhibitory concentrations of these organisms by several orders of magnitude."( Pharmacology of the allylamines.
Birnbaum, JE, 1990
)
0.6
"90 (SD) and the mean relative bioavailability of the mixture was slightly above 100%."( Analgesic effect and bioavailability of oral ketogan given as tablets or mixture to patients with chronic pain of malignant origin.
Kjaer, M; Nielsen, H, 1988
)
0.27
" Toxicokinetic study showed a very rapid absorption rate and short half-lives (less than 1 h) for those organs which reasonably fit a toxicokinetic one-compartment model."( Allylamine cardiovascular toxicity: V. Tissue distribution and toxicokinetics after oral administration.
Boor, PJ, 1985
)
1.71
"The basic pharmacokinetics and oral bioavailability of ketobenmidone have been studied in 6 patients after surgery."( Clinical pharmacokinetics and oral bioavailability of ketobemidone.
Anderson, P; Arnér, S; Bondesson, U; Boréus, LO; Hartvig, P, 1980
)
0.26
"The pharmacokinetic constants and rectal bioavailability of the narcotic analgesic ketobemidone were determined in six male patients after surgery."( Clinical pharmacokinetics of ketobemidone. Its bioavailability after rectal administration.
Anderson, P; Arnér, S; Bondesson, U; Boréus, LO; Hartvig, P, 1981
)
0.26
"Colesevelam HCl had no significant effect on fenofibrate bioavailability when administered either concomitantly with fenofibrate or 4 hours after fenofibrate."( Effect of colesevelam HCl on single-dose fenofibrate pharmacokinetics.
Baker, BA; Jones, MR; Mathew, P, 2004
)
0.32
" Furthermore, it provides a highly efficient cellular uptake and excellent bioavailability in vitro and enables a deep penetration during transfollicular delivery in vivo."( Transdermal platform for the delivery of the antifungal drug naftifine hydrochloride based on porous vaterite particles.
Abalymov, A; Atkin, V; Gusliakova, O; Kozlova, A; Lengert, E; Morrison, A; Nechaeva, O; Svenskaya, Y; Tuchin, V; Verkhovskii, R, 2021
)
0.62

Dosage Studied

ExcerptRelevanceReference
" In dose-response experiments, rat hearts perfused with allylamine (10-30 mM) or acrolein (0."( Allylamine and acrolein toxicity in perfused rat hearts.
Anderson, PG; Boor, PJ; Sklar, JL, 1991
)
1.97
" The patients were six days in hospital and were dosed two days with tablets, two days with mixture and finally another two days with tablets."( Analgesic effect and bioavailability of oral ketogan given as tablets or mixture to patients with chronic pain of malignant origin.
Kjaer, M; Nielsen, H, 1988
)
0.27
" The low oral bioavailability and rapid elimination of ketobemidone demonstrated in this study suggest that the usual dosage recommendation for oral Ketogin (ketobemidone 5--10 mg every 6--7 h) in patients with severe pain is too low."( Clinical pharmacokinetics and oral bioavailability of ketobemidone.
Anderson, P; Arnér, S; Bondesson, U; Boréus, LO; Hartvig, P, 1980
)
0.26
"5 ng/ml of tyramine in 1 ml of human plasma and is thus suitable for monoamine oxidase inhibitor studies involving oral dosing with tyramine."( Measurement of tyramine in human plasma, utilising ion-pair extraction and high-performance liquid chromatography with amperometric detection.
Brown, MJ; Causon, RC, 1984
)
0.27
" Dosing regimen evaluations indicate that colesevelam is effective at both once per day and twice daily dosing and that concurrent administration of colesevelam with hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins), specifically lovastatin, does not alter the absorption of the statin."( Colesevelam hydrochloride: a non-absorbed, polymeric cholesterol-lowering agent.
Davidson, MH; Dicklin, MR; Kleinpell, RM; Maki, KC, 2000
)
0.31
"0001) when colesevelam and lovastatin were dosed together or dosed apart, respectively."( Low-dose combination therapy with colesevelam hydrochloride and lovastatin effectively decreases low-density lipoprotein cholesterol in patients with primary hypercholesterolemia.
Burke, SK; Davidson, MH; Donovan, JM; Hunninghake, D; Isaacsohn, J; McKenney, J; Toth, P; Weiss, S, 2001
)
0.31
" Colesevelam appears to be more cost-effective than the packet dosage form of the brand formulation of the older bile acid resins."( Colesevelam hydrochloride: a novel bile acid-binding resin.
Aldridge, MA; Ito, MK,
)
0.13
"The pharmacology, pharmacodynamics, clinical efficacy, drug interactions, adverse effects, and dosage and administration of colesevelam hydrochloride are reviewed."( Colesevelam hydrochloride.
Steinmetz, KL, 2002
)
0.31
" Ezetimibe has a relatively flat dose-response curve and titration is not required."( Hypolipidemic therapy and cholesterol absorption.
Farmer, JA; Manhas, A, 2004
)
0.32
" In a mouse model of inflammatory leukocyte trafficking oral dosing with LJP 1586 resulted in significant dose-dependent inhibition of neutrophil accumulation, with an effect comparable to that of anti-leukocyte function-associated antigen-1 antibody."( Anti-inflammatory effects of LJP 1586 [Z-3-fluoro-2-(4-methoxybenzyl)allylamine hydrochloride], an amine-based inhibitor of semicarbazide-sensitive amine oxidase activity.
Gao, H; Huang, L; Jones, DS; Kessler, C; Linnik, MD; Macdonald, MT; Miller, A; O'Rourke, AM; Podar, EM; Scheyhing, K; Ton-Nu, HT; Wang, EY, 2008
)
0.58
"The purpose of this article was to review the pharmacology, pharmacokinetics, efficacy, adverse effects and tolerability, drug-drug interactions, contraindications/precautions, dosage and administration, pharmacoeconomics, and the overall role of colesevelam in the management of adult patients with type 2 DM."( Colesevelam hydrochloride for the treatment of type 2 diabetes mellitus.
Gates, BJ; Levien, TL; Neumiller, JJ; Setter, SM; Sonnett, TE, 2009
)
0.35
" The maximum dosage of colesevelam (3."( A 50-week extension study on the safety and efficacy of colesevelam in adults with primary hypercholesterolemia.
Davidson, MH; Donovan, JM; Jones, MR; Misir, S, 2010
)
0.36
" Several compounds elicited this increase in enzyme activity over a relatively wide dosage range."( Rapid assembly of a library of lipophilic iminosugars via the thiol-ene reaction yields promising pharmacological chaperones for the treatment of Gaucher disease.
Goddard-Borger, ED; Mahuran, DJ; Tropak, MB; Tysoe, C; Withers, SG; Yonekawa, S, 2012
)
0.38
" Twelve subjects were dosed daily (6 with naftifine cream, 2% and 6 with naftifine gel, 2%)."( Detection and relevance of naftifine hydrochloride in the stratum corneum up to four weeks following the last application of naftifine cream and gel, 2%.
Fleischer, AB; Hardas, B; Olayinka, B; Plaum, S; Verma, A, 2013
)
0.39
" For the colesevelam coadministration periods, 3,750 mg once daily was dosed throughout the pharmacokinetic sampling period."( The effects of colesevelam HCl on the single-dose pharmacokinetics of glimepiride, extended-release glipizide, and olmesartan medoxomil.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014
)
0.4
" Colesevelam (3750mg once daily) was dosed throughout the pharmacokinetic sampling period."( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014
)
0.4
" Wistar rats were dosed once with either isoproterenol (1."( miR-21-5p as a potential biomarker of inflammatory infiltration in the heart upon acute drug-induced cardiac injury in rats.
De Ron, P; Fleming, A; Fleurance, R; Gryshkova, V; McGhan, P; Nogueira da Costa, A; Valentin, JP, 2018
)
0.48
" Poor readability of prescription/over-the-counter (OTC) antifungals may contribute to poor adherence, due to the patient not fully understanding the purpose, importance, and dosage of their antifungal medicine."( Improving health literacy of antifungal use-Comparison of the readability of antifungal medicines information from Australia, EU, UK, and US of 16 antifungal agents across 5 classes (allylamines, azoles, echinocandins, polyenes, and others).
Millar, BC; Moore, JE; Tang, KWK, 2023
)
1.1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
alkylamineAny primary amine in which the substituent attached to nitrogen is an alkyl group.
[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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency25.11890.003245.467312,589.2998AID2517
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency7.51230.011212.4002100.0000AID1030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50 (µMol)500.00000.00040.764912.5000AID127347
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50 (µMol)500.00000.00071.979812.5000AID127347
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID127347Inhibitory activity against rat brain mitochondrial Monoamine oxidase1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Enzyme-activated irreversible inhibitors of monoamine oxidase: phenylallylamine structure-activity relationships.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (697)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990147 (21.09)18.7374
1990's116 (16.64)18.2507
2000's187 (26.83)29.6817
2010's223 (31.99)24.3611
2020's24 (3.44)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.79

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index56.79 (24.57)
Research Supply Index6.74 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index94.97 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials112 (15.26%)5.53%
Reviews99 (13.49%)6.00%
Case Studies18 (2.45%)4.05%
Observational0 (0.00%)0.25%
Other505 (68.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]