General Information of Drug (ID: DM7ADGX)

Drug Name
Carfentanil Drug Info
Synonyms
CARFENTANIL; Carfentanyl; Carfentanila; Carfentanilum; Wildnil; 59708-52-0; Carfentanil [INN]; Carfentanila [Spanish]; UNII-LA9DTA2L8F; Carfentanilum [INN-Latin]; Carfentanila [INN-Spanish]; Methyl 1-phenylethyl-4-(N-phenylpropionamido)isonipecotate; CHEBI:61084; Methyl 4-(N-propionyl-N-phenylamino)-1-(2-phenylethyl)-4-piperidine-carboxylate; Methyl 4-(N-(1-oxopropyl)-N-phenylamino)-1-(2-phenylethyl)-4-piperidinecarboxylate; 4-((1-Oxopropyl)phenylamino)-1-(2-phenylethyl)-4-piperidinecarboxylic acid methyl ester
Cross-matching ID
PubChem CID
62156
ChEBI ID
CHEBI:61084
CAS Number
CAS 59708-52-0
TTD Drug ID
DM7ADGX
INTEDE Drug ID
DR1865

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [3]
Progesterone DMUY35B Premature labour JB00 Approved [4]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [6]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [7]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [8]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [9]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [10]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [4]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Opioid receptor mu (MOP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Buprenorphine DMPRI8G Pain MG30-MG3Z Approved [12]
Morphine DMRMS0L Chronic pain MG30 Approved [13]
Hydromorphone DMHP21E Pain MG30-MG3Z Approved [14]
Tapentadol hydrochloride DMXLSH3 Acute pain MG31 Approved [15]
Fentanyl DM8WAHT Analgesia MB40.8 Approved [16]
Alfentanil DMVO0UB Anaesthesia 9A78.6 Approved [17]
Naloxegol DML0B41 Opioid-induced constipation DB32.1 Approved [18]
Eluxadoline DMYZ0P1 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [19]
Nalfurafine hcl DMA9DHW Uremic pruritus EC90.10 Approved [20]
Oxycodone DMXLKHV Pain MG30-MG3Z Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Codeine DMJX6ZG Pain MG30-MG3Z Approved [22]
Hydromorphone DMHP21E Pain MG30-MG3Z Approved [23]
Loperamide DMOJZQ9 Diarrhea ME05.1 Approved [24]
Eluxadoline DMYZ0P1 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [19]
Oxycodone DMXLKHV Pain MG30-MG3Z Approved [25]
Butorphanol DM5KYPJ Pain MG30-MG3Z Approved [22]
TPM-1/Morphine DM4R23C Pain MG30-MG3Z Phase 2 [26]
Met-enkephalin DMSZFTP Pain MG30-MG3Z Phase 2 [27]
AZD-2327 DM8FZOG Anxiety disorder 6B00-6B0Z Phase 2 [28]
ADL-5747 DMMUPTN Pain MG30-MG3Z Phase 2 [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nalbuphine DMOSQGU Pain MG30-MG3Z Approved [30]
Nalfurafine hcl DMA9DHW Uremic pruritus EC90.10 Approved [20]
Chloroxine DMFZBMQ Erythema ME64.0 Approved [31]
Dezocine DMJDB0Y Pain MG30-MG3Z Approved [32]
Asimadoline DMND3AB Diarrhea-predominant irritable bowel syndrome DD91.01 Phase 3 [33]
Difelikefalin DMHZBEO Pruritus EC90 Phase 3 [34]
PHN-131 DM1SV8I Pain MG30-MG3Z Phase 2/3 [35]
CR-845 DMJYTUQ Pain MG30-MG3Z Phase 2/3 [36]
TPM-1/Morphine DM4R23C Pain MG30-MG3Z Phase 2 [26]
Apadoline DM1B8IT Pain MG30-MG3Z Phase 2 [37]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Opioid receptor delta (OPRD1) TT27RFC OPRD_HUMAN Agonist [1]
Opioid receptor kappa (OPRK1) TTQW87Y OPRK_HUMAN Agonist [1]
Opioid receptor mu (MOP) TTKWM86 OPRM_HUMAN Agonist [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [2]
Acid cholesteryl ester hydrolase (LIPA) DE2PJF5 LICH_HUMAN Substrate [2]

References

1 Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.
2 Metabolism of carfentanil, an ultra-potent opioid, in human liver microsomes and human hepatocytes by high-resolution mass spectrometry. AAPS J. 2016 Nov;18(6):1489-1499.
3 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
4 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
5 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
6 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
7 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
8 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
9 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
10 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
11 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
12 Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
13 Antianalgesia: stereoselective action of dextro-morphine over levo-morphine on glia in the mouse spinal cord.J Pharmacol Exp Ther.2005 Sep;314(3):1101-8.
14 Clinical pipeline report, company report or official report of signaturerx.
15 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
16 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
17 Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87.
18 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
19 Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
20 Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
21 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 319).
22 Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16.
23 Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. J Med Chem. 2004 Mar 11;47(6):1400-12.
24 Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8.
25 Oxycodone: a pharmacological and clinical review. Clin Transl Oncol. 2007 May;9(5):298-307.
26 Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior. Anesthesiology. 2011 December; 115(6): 1363-1381.
27 Delta-opioid receptor agonists inhibit neuromuscular transmission in human colon. Eur J Pharmacol. 1994 Sep 1;262(1-2):33-9.
28 Preclinical pharmacology of AZD2327: a highly selective agonist of the delta-opioid receptor. J Pharmacol Exp Ther. 2011 Jul;338(1):195-204.
29 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 317).
30 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
31 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
32 Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3.
33 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
34 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
35 Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J Pharmacol Exp Ther. 1988 Jan;244(1):391-402.
36 Peptide Kappa Opioid Receptor Ligands: Potential for Drug Development. AAPS J. 2009 June; 11(2): 312-322.
37 Novel developments with selective, non-peptidic kappa-opioid receptor agonists. Expert Opin Investig Drugs. 1997 Oct;6(10):1351-68.