Page last updated: 2024-12-06

carfentanil

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

Description

carfentanil : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of methyl 4-anilino-1-(2-phenylethyl)piperidine-4-carboxylate with propanoic acid. [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]

Cross-References

ID SourceID
PubMed CID62156
CHEMBL ID290429
CHEBI ID61084
SCHEMBL ID116222
MeSH IDM0067592

Synonyms (57)

Synonym
carfentanila
carfentanilum
methyl 1-(2-phenylethyl)-4-[phenyl(propionyl)amino]piperidine-4-carboxylate
brn 0456976
methyl 4-(n-propionyl-n-phenylamino)-1-(2-phenylethyl)-4-piperidine-carboxylate
carfentanil [inn]
carfentanila [spanish]
methyl 4-(n-(1-oxopropyl)-n-phenylamino)-1-(2-phenylethyl)-4-piperidinecarboxylate
carfentanila [inn-spanish]
dea no. 9743
4-((1-oxopropyl)phenylamino)-1-(2-phenylethyl)-4-piperidinecarboxylic acid methyl ester
methyl 1-phenylethyl-4-(n-phenylpropionamido)isonipecotate
carfentanilum [inn-latin]
4-piperidinecarboxylic acid, 4-((1-oxopropyl)phenylamino)-1-(2-phenylethyl)-, methyl ester, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
4-piperidinecarboxylic acid, 4((1-oxopropyl)phenylamino)-1-(2-phenylethyl)-, methyl ester
wildnil
carfentanil
r-31833
DB01535
carfentanyl
4-carbomethoxyfentanyl
CHEMBL290429 ,
chebi:61084 ,
r 31833
(4-carbomethoxy fentanyl)
59708-52-0
D07620
carfentanil (inn)
AKOS005067304
1-phenethyl-4-(phenyl-propionyl-amino)-piperidine-4-carboxylic acid methyl ester(carefentanil)
bdbm50012477
carfentanil1-phenethyl-4-(phenyl-propionyl-amino)-piperidine-4-carboxylic acid methyl ester
1-phenethyl-4-(phenyl-propionyl-amino)-piperidine-4-carboxylic acid methyl ester
r31833
(4-methoxycarbonyl)fentanyl
4-methoxycarbonylfentanyl
4-methoxycarbonyl fentanyl
methyl 1-phenethyl-4-(n-phenylpropionamido)isonipecotate
la9dta2l8f ,
unii-la9dta2l8f
hsdb 8376
EPITOPE ID:153509
4-piperidinecarboxylic acid, 4-((1-oxopropyl)phenylamino)-1-(2-phenylethyl)-, methyl ester
SCHEMBL116222
methyl 1-(2-phenylethyl)-4-(propionylanilino)-4-piperidinecarboxylate #
YDSDEBIZUNNPOB-UHFFFAOYSA-N
DTXSID40208427 ,
gtpl10040
methyl 1-(2-phenylethyl)-4-(phenyl-propanoylamino)piperidine-4-carboxylate
Q423386
methyl 1-(2-phenylethyl)-4-(n-propanoylanilino)piperidine-4-carboxylate
methyl 1-(2-phenylethyl)-4-(n-phenylpropanamido)piperidine-4-carboxylate
84K ,
methyl 1-(2-phenylethyl)-4-(phenyl(propionyl)amino)piperidine-4-carboxylate
carfentanilum (latin)
dtxcid60130918
carfentanilo

Research Excerpts

Overview

Carfentanil (CRF) is an extremely potent opioid capable of inducing fatal respiratory depression. It presents a serious threat to public health and road safety due to its presence in the illicit drug supply, the potency of the drug and instances of use prior to the operation of a motor vehicle. Carfenil is a synthetic opioid approximately 10,000 times as powerful as morphine.

ExcerptReferenceRelevance
"Carfentanil is a synthetic opioid significantly more potent than clinically prescribed fentanyl. "( Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
Cooper, NJ; Feasel, MG; Goralski, TDP; Hsu, FL; Kong, L; Myslinski, JM; Rose, T; Roughley, N; Timperley, CM; Walz, AJ, 2019
)
2.2
"Carfentanil is a potent opioid with no medical use in humans; it presents a serious threat to public health and road safety due to its presence in the illicit drug supply, the potency of the drug and instances of use prior to the operation of a motor vehicle. "( Carfentanil Blood Concentrations in Impaired Driving Investigations in Ontario, Canada.
Elliot, M; Rajotte, JW; Wallage, HR, 2022
)
3.61
"Carfentanil is a β-arrestin-biased opioid drug at the μ receptor. "( Carfentanil is a β-arrestin-biased agonist at the μ opioid receptor.
Bailey, CP; Bancroft, S; Groom, S; Henderson, G; Kelly, E; Ramos-Gonzalez, N; Sessions, RB; Sutcliffe, KJ, 2023
)
3.8
"Carfentanil is an ultra-potent synthetic opioid. "( The Synthesis of Biphasic Metabolites of Carfentanil.
Chen, R; He, S; Hu, J; Liao, P; Liu, W; Wang, J; Xue, S; Zhao, X, 2023
)
2.62
"Carfentanil (CRF) is an extremely potent opioid capable of inducing fatal respiratory depression. "( Changes in murine respiratory dynamics induced by aerosolized carfentanil inhalation: Efficacy of naloxone and naltrexone.
McCranor, BJ; Pierce, SA; Racine, MC; Sciuto, AM; Tressler, J; Tuet, WY; Wong, B, 2019
)
2.2
"Carfentanil is a synthetic opioid with an estimated potency that is 10,000 times more than that of morphine and 100 times more than that of fentanyl. "( Higher naloxone dosing may be required for opioid overdose.
Bardsley, R, 2019
)
1.96
"Carfentanil is a synthetic opioid approximately 10,000 times as powerful as morphine. "( Carfentanil Use in a Patient Undergoing Treatment for Substance Use Disorder.
Antara, JP; Banks, JF; Bollini, SM; Hobbs, GA; Tuzel, T, 2020
)
3.44
"Carfentanil is a synthetic opioid restricted to veterinary use due to its potency. "( Percutaneous absorption of Carfentanil in vitro.
Dalton, C; Graham, S; Pritchard, S; Watkins, R, 2021
)
2.36
"Carfentanil is an ultra-potent opioid with an analgesic potency 10,000 times that of morphine but has received little scientific investigation. "( Identification of human cytochrome P450 isozymes involved in the oxidative metabolism of carfentanil.
Kong, L; Walz, AJ, 2021
)
2.29
"Carfentanil is a fentanyl analog frequently used in large animal veterinary medicine. "( Fatalities Involving Carfentanil and Furanyl Fentanyl: Two Case Reports.
Brogan, SC; Hair, LS; Pearson, JM; Smyth, BC; Strauch Rivers, SR; Swanson, DM; Vaccaro, SL; Ventoso, AD, 2017
)
2.22
"Carfentanil is a mu (μ) opioid receptor agonist and is estimated to be ~10,000 times more potent than morphine in animal (non-human) models. "( Detection of Carfentanil by LC-MS-MS and Reports of Associated Fatalities in the USA.
Behonick, GS; Shanks, KG, 2017
)
2.27
"Carfentanil is an ultra-potent opioid requiring a method with adequate sensitivity for detection in blood specimens from impairment cases."( Carfentanil in Impaired Driving Cases and the Importance of Drug Seizure Data.
Alford, I; Tiscione, NB, 2018
)
2.64
"Carfentanil is a synthetic fentanyl analogue approved for veterinary use. "( Carfentanil: a narrative review of its pharmacology and public health concerns.
Juurlink, DN; Leen, JLS, 2019
)
3.4
"Carfentanil is an ultra-potent synthetic opioid. "( Metabolism of Carfentanil, an Ultra-Potent Opioid, in Human Liver Microsomes and Human Hepatocytes by High-Resolution Mass Spectrometry.
Feasel, MG; Huestis, MA; Kristovich, RL; Nilles, JM; Pang, S; Wohlfarth, A, 2016
)
2.24
"11C-carfentanil is a radiopharmaceutical that selectively binds the mu-opiate receptor of the central nervous system. "( Dosimetry of 11C-carfentanil, a micro-opioid receptor imaging agent.
Divgi, C; Freifelder, R; Karp, J; Lerman, C; Newberg, AB; Ray, R; Saffer, J; Scheuermann, J; Schmitz, A; Wintering, N, 2009
)
1.25
"[11C]Carfentanil is a potent opioid agonist currently in use as a specific PET (position emission tomography) scan radioligand for brain mu opioid receptors. "( Mu opiate receptors are selectively labelled by [3H]carfentanil in human and rat brain.
Bullock, A; Dannals, RF; Frost, JF; Kuhar, MJ; Leonhardt, S; Lyon, RA; Price, DL; Rydelek, LT; Struble, RG; Titeler, M, 1989
)
1.04
"Carfentanil is a potent, synthetic opiate that binds to mu opiate receptors with very high affinity (KI = 0.051 nM, 37 degrees C). "( Imaging opiate receptors in the human brain by positron tomography.
Burns, HD; Dannals, RF; Frost, JJ; Links, JM; McPherson, RW; Ravert, HT; Rosenbaum, AE; Wagner, HN; Wilson, AA; Wong, DF,
)
1.57

Effects

Carfentanil for example has an estimated potency 10,000 times greater than morphine and thus is highly dangerous for human use. CarfENTanil has a half-life of 7.7 hr, whereas naltrexone has a much shorter half- life of 3.7hr.

Carfentanil-xylazine (CX) has been the primary drug combination used for immobilizing free-ranging ungulates in Alaska, US since 1986. CarfENTanil for example has an estimated potency 10,000 times greater than morphine and thus is highly dangerous for human use.

ExcerptReferenceRelevance
"Carfentanil for example has an estimated potency 10,000 times greater than morphine and thus is highly dangerous for human use."( A Highly Efficacious Carfentanil Vaccine That Blunts Opioid-Induced Antinociception and Respiratory Depression.
Blake, S; Bremer, PT; Ellis, B; Eubanks, LM; Janda, KD; Natori, Y, 2021
)
1.66
"Carfentanil has a half-life of 7.7 hr, whereas naltrexone has a much shorter half-life of 3.7 hr."( Pharmacokinetics and pharmacodynamics of carfentanil and naltrexone in female common eland (Taurotragus oryx).
Carpenter, JW; Cole, A; Dresser, BL; Hunter, RP; Isaza, R; Koch, DE; Mutlow, A, 2006
)
1.32
"Carfentanil for example has an estimated potency 10,000 times greater than morphine and thus is highly dangerous for human use."( A Highly Efficacious Carfentanil Vaccine That Blunts Opioid-Induced Antinociception and Respiratory Depression.
Blake, S; Bremer, PT; Ellis, B; Eubanks, LM; Janda, KD; Natori, Y, 2021
)
1.66
"Carfentanil-xylazine (CX) has been the primary drug combination used for immobilizing free-ranging ungulates in Alaska, US since 1986. "( THIAFENTANIL-AZAPERONE-XYLAZINE AND CARFENTANIL-XYLAZINE IMMOBILIZATIONS OF FREE-RANGING CARIBOU (RANGIFER TARANDUS GRANTI) IN ALASKA, USA.
Arnemo, JM; Beckmen, KB; Bentzen, TW; Demma, DJ; Lian, M, 2016
)
2.15
"Carfentanil has a half-life of 7.7 hr, whereas naltrexone has a much shorter half-life of 3.7 hr."( Pharmacokinetics and pharmacodynamics of carfentanil and naltrexone in female common eland (Taurotragus oryx).
Carpenter, JW; Cole, A; Dresser, BL; Hunter, RP; Isaza, R; Koch, DE; Mutlow, A, 2006
)
1.32

Toxicity

ExcerptReferenceRelevance
" We observed no adverse clinical effects in elk receiving < or = 500 mg naltrexone/mg carfentanil."( Efficacy and safety of naltrexone hydrochloride for antagonizing carfentanil citrate immobilization in captive Rocky Mountain elk (Cervus elaphus nelsoni).
Lance, WR; Miller, MW; Wild, MA, 1996
)
0.76

Pharmacokinetics

ExcerptReferenceRelevance
" This study examined the duration of action of BUP at microORs and correlations with pharmacokinetic and pharmacodynamic outcomes in 10 heroin-dependent volunteers."( Buprenorphine duration of action: mu-opioid receptor availability and pharmacokinetic and behavioral indices.
Bueller, J; Chang, Y; Greenwald, M; Johanson, CE; Kilbourn, M; Koeppe, R; Moody, DE; Zubieta, JK, 2007
)
0.34
"Together with our previous findings, it appears that microOR availability predicts changes in pharmacokinetic and pharmacodynamic measures and that about 50%-60% BUP occupancy is required for adequate withdrawal symptom suppression (in the absence of other opioids) and HYD blockade."( Buprenorphine duration of action: mu-opioid receptor availability and pharmacokinetic and behavioral indices.
Bueller, J; Chang, Y; Greenwald, M; Johanson, CE; Kilbourn, M; Koeppe, R; Moody, DE; Zubieta, JK, 2007
)
0.34
"The pharmacokinetic parameters of carfentanil and naltrexone were determined in the common eland (Taurotragus oryx)."( Pharmacokinetics and pharmacodynamics of carfentanil and naltrexone in female common eland (Taurotragus oryx).
Carpenter, JW; Cole, A; Dresser, BL; Hunter, RP; Isaza, R; Koch, DE; Mutlow, A, 2006
)
0.88

Compound-Compound Interactions

ExcerptReferenceRelevance
"Anaesthesia in guinea pigs with a new highly potent and short-acting analgesic, carfentanyl (R 33799), combined with the hypnotic, etomidat (R 26490), is reported."( A new highly potent and short-acting analgesic, carfentanyl (R 33799), in combination with the hypnotic agent, etomidat (R 26490), as a method of anaesthesia in guinea pigs.
Blümel, G; Erhardt, W; Fritsch, R; Neumann, G; Oberhuber, B, 1980
)
0.26

Dosage Studied

Eight domestic goats (Capra hircus) were anesthetized with a combination of carfentanil citrate and detomidine HCl each at a dosage of 60 micrograms/kg, mixed with an equal volume. The lowest dosage used, the lowest dosage of 0.8micrograms carfENTanil/kg was very excited during induction and required intravenous (IV) ketamine to permit safe examination.

ExcerptRelevanceReference
" Further investigations need to be done to establish the most appropriate dosage rates for these preparations in ostriches."( Ostrich (Struthio camelus) immobilisation using carfentanil and xylazine and reversal with yohimbine and naltrexone.
Malan, JH; Quandt, SK; Raath, JP, 1992
)
0.54
" When the C1 antibody was combined with an iodinated analog to fentanyl, good detectability of alpha-methylfentanyl and 3-methylfentanyl, in terms of fentanyl equivalents, was obtained from urine samples of dosed mares."( Pharmacologic effects and detection methods of methylated analogs of fentanyl in horses.
Blake, JW; Tai, CL; Tai, HH; Tobin, T; Weckman, TJ; Woods, WE, 1989
)
0.28
" The dosage rates of the immobilization combinations for mammmals, birds and reptiles are presented in tabular form."( [Practical advice concerning the immobilization of wild and zoo animals].
von Hegel, G; Wiesner, H, 1985
)
0.27
" The use of the newly developed piperidine derivative R 33799 at weight treated dosage levels can be strongly recommended for the immobilisation of hartebeest."( On the immobilization of hartebeest and kob in Upper Volta.
Dräger, N; Küpper, W; Mehlitz, D; Zillmann, U, 1981
)
0.26
" Although it was possible that the clinical findings in these horses may have resulted from use of an inadequate dosage of carfentanil or xylazine, or both, analysis of the results more likely indicated that domestic and exotic horses may respond differently to carfentanil, and domestic horses may not be a good model for use in studies of carfentanil."( Complications with the use of carfentanil citrate and xylazine hydrochloride to immobilize domestic horses.
Carpenter, JW; Leith, DE; Shaw, ML, 1995
)
0.79
"8 micrograms carfentanil/kg, the lowest dosage used, was very excited during induction and required intravenous (IV) ketamine to permit safe examination."( Immobilization of black bears (Ursus americanus) with orally administered carfentanil citrate.
Clyde, VL; Ramsay, EC; Sleeman, JM, 1995
)
0.89
"Although the cardiopulmonary effects of carfentanil occurred more rapidly, these effects were similar in magnitude for etorphine and carfentanil over the evaluated dosage range."( Comparative cardiopulmonary effects of intramuscularly administered etorphine and carfentanil in goats.
Buss, D; Heard, DJ; Kollias, GV; Nichols, WW, 1996
)
0.79
" Fifteen min after each elk became recumbent, we administered naltrexone HCl (25% of dose intravenously, 75% subcutaneously) dosed at 0 (control), 25, 50, or 100 mg/mg carfentanil; after an additional 15 min of immobilization, controls received 500 mg naltrexone HCl/mg carfentanil."( Efficacy and safety of naltrexone hydrochloride for antagonizing carfentanil citrate immobilization in captive Rocky Mountain elk (Cervus elaphus nelsoni).
Lance, WR; Miller, MW; Wild, MA, 1996
)
0.73
"The carfentamil-xylazine combination at the dosage used induced hypoxemia, pronounced arterial hypertension, and significant increase in plasma norepinephrine and decrease in plasma 3,4-dihydroxyphenylacetic acid concentrations in bongo antelopes."( Effects of a carfentanil-xylazine combination on cardiopulmonary function and plasma catecholamine concentrations in female bongo antelopes.
Citino, SB; Dawson, R; Schumacher, J, 1997
)
0.67
" Pharmacokinetics and mu-opioid receptor occupancy of nalmefene after single and repeated dosing over 7 days was studied in 12 healthy subjects."( Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing.
Aalto, S; Hagelberg, N; Hietala, J; Ingman, K; Juhakoski, A; Kallio, A; Karhuvaara, S; Någren, K; Oikonen, V; Scheinin, H, 2005
)
0.33
" A fixed ratio of 1 mg CAR:10 mg XYL intramuscularly was used, increasing or decreasing the dosage until the optimal dosage (defined by an induction time < 3 min and PaCO(2)< 60 mmHg) was reached for each animal."( Determination and evaluation of an optimal dosage of carfentanil and xylazine for the immobilization of white-tailed deer (Odocoileus virginianus).
Miller, KV; Osborn, DA; Ramsay, EC; Schumacher, J; Storms, TN; Zagaya, N, 2005
)
0.58
"Using a crossover design, the effects of the addition of ketamine to a previously determined optimal hand-injected immobilization dosage of carfentanil/xylazine were evaluated in 11 adult white-tailed deer (Odocoileus virginianus)."( Effects of ketamine on carfentanil and xylazine immobilization of white-tailed deer (Odocoileus virginianus).
Miller, KV; Osborn, DA; Ramsay, EC; Schumacher, J; Storms, TN, 2006
)
0.85
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
mu-opioid receptor agonistA compound that exhibits agonist activity at the mu-opioid receptor.
opioid analgesicA narcotic or opioid substance, synthetic or semisynthetic agent producing profound analgesia, drowsiness, and changes in mood.
tranquilizing drugA traditional grouping of drugs said to have a soothing or calming effect on mood, thought or behaviour.
[role 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]

Drug Classes (4)

ClassDescription
piperidines
methyl esterAny carboxylic ester resulting from the formal condensation of a carboxy group with methanol.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
tertiary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
[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]

Pathways (1)

PathwayProteinsCompounds
Carfentanil Action Pathway3111

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00320.00000.60689.2330AID148442; AID150398
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00020.00000.38458.6000AID150398; AID151894
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki0.00030.00000.18683.9500AID150398
Mu-type opioid receptorHomo sapiens (human)Ki0.00000.00000.419710.0000AID150845
Delta-type opioid receptorHomo sapiens (human)Ki0.00330.00000.59789.9300AID150088
Kappa-type opioid receptorHomo sapiens (human)Ki0.04310.00000.362410.0000AID148708
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00000.00000.32639.4000AID1611652
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID1188145Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID150845Binding affinity against Opioid receptor mu 12000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
AID1188144Displacement of [3H]DSLET from delta opioid receptor in rat brain membranes2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID1611650Drug metabolism in human liver microsomes at 10 uM assessed as rac-methyl 1-(2-hydroxy-2-phenylethyl)-4-(N-phenylpropionamido)piperidine-4-carboxylate metabolite formation incubated for 5 mins in presence of NADPH and measured after 2 hrs by UHPLC-HRMS an2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
AID73902Inhibition of electrically evoked contraction in guinea pig ileum determined in vitro1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgetics.
AID150088Binding affinity against Opioid receptor delta 12000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
AID174621Duration of analgesic effect calculated using in vivo rat tail withdrawal assay.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgetics.
AID1188147Selectivity ratio of Ki for kappa opioid receptor in guinea pig brain membranes to Ki for mu opioid receptor in rat brain membranes2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID151894Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 11990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID177922Analgesic effect calculated using in vivo rat tail withdrawal assay.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgetics.
AID150398Inhibition of [3H]diprenorphine binding to rat brain membrane opioid receptors;(T= total opioid receptor family)1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID177756Analgesic activity at 1 min following injection at 1 mg/kg into the lateral tail vein of the rat (55 degree Centigrade hot plate assay)1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.
AID1188151Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID1611651Drug metabolism in human liver microsomes at 10 uM assessed as methyl 4-(N-phenylpropionamido)piperidine-4-carboxylate metabolite formation incubated for 5 mins in presence of NADPH and measured after 2 hrs by UHPLC-HRMS analysis relative to control2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
AID1611652Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
AID1611649Drug metabolism in human liver microsomes at 10 uM assessed as Cis/trans-4-(methoxycarbonyl)-1-phenethyl-4-(N-phenylpropionamido)piperidine 1-oxide metabolite formation incubated for 5 mins in presence of NADPH and measured after 2 hrs by UHPLC-HRMS analy2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
AID148708Binding affinity against Opioid receptor kappa 12000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
AID149543Opioid receptor kappa 1 apparent binding constant from guinea pig cerebellum using [3H]diprenorphine binding assay1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID1188148Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID1188146Selectivity ratio of Ki for delta opioid receptor in rat brain membranes to Ki for mu opioid receptor in rat brain membranes2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID1611647Drug metabolism in human liver microsomes at 10 uM assessed as methyl 4-(3-hydroxy-N-phenylpropanamido)-1-phenethylpiperidine-4-carboxylate metabolite formation incubated for 5 mins in presence of NADPH and measured after 2 hrs by UHPLC-HRMS analysis rela2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
AID148442Opioid receptor kappa 1 apparent binding constant from rat brain membranes using [3H]DADLE binding assay1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID1188143Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
AID1611646Drug metabolism in human liver microsomes at 10 uM assessed as methyl 1-(4-hydroxyphenethyl)-4-(N-phenylpropionamido)piperidine-4-carboxylate metabolite formation incubated for 5 mins in presence of NADPH and measured after 2 hrs by UHPLC-HRMS analysis re2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
AID1611648Drug metabolism in human liver microsomes at 10 uM assessed as methyl 1-(2-oxo-2-phenylethyl)-4-(N-phenylpropionamido)piperidine-4-carboxylate metabolite formation incubated for 5 mins in presence of NADPH and measured after 2 hrs by UHPLC-HRMS analysis r2019ACS medicinal chemistry letters, Nov-14, Volume: 10, Issue:11
Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (261)

TimeframeStudies, This Drug (%)All Drugs %
pre-199029 (11.11)18.7374
1990's41 (15.71)18.2507
2000's50 (19.16)29.6817
2010's104 (39.85)24.3611
2020's37 (14.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 78.47

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 Index78.47 (24.57)
Research Supply Index5.70 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index138.47 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (78.47)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials27 (9.96%)5.53%
Reviews13 (4.80%)6.00%
Case Studies13 (4.80%)4.05%
Observational0 (0.00%)0.25%
Other218 (80.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Detecting Neuromolecular Risk Factors for Obesity [NCT03106688]60 participants (Anticipated)Interventional2017-04-04Active, not recruiting
A Phase 1, Open-label Trial to Evaluate Target Occupancy of CVL-354 at Kappa Opioid and Mu Opioid Receptors in Brain Following Single Oral Doses in Healthy Participants Using Positron Emission Tomography [NCT05547542]Phase 124 participants (Anticipated)Interventional2023-03-01Recruiting
Effects of Smoking on Opioid Receptor Binding Using [(11)C]Carfentanil: An Imaging PET Study [NCT00618631]Phase 126 participants (Actual)Interventional2008-01-17Completed
Pilot Study of a Multi-System Analysis of Opioid Receptor Binding [NCT05528848]Phase 160 participants (Anticipated)Interventional2022-09-20Recruiting
Towards Individualized Deep Brain Stimulation Treatment of Chronic Neuropathic Pain [NCT01899170]Phase 23 participants (Actual)Interventional2014-04-01Terminated(stopped due to Device for multi coil TMS no longer supported)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]