About: Carfentanil     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...generalReferences
  • # Wax PM, Becker CE, Curry SC: Unexpected "gas" casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12712038 (en)
http://linked.open...gy/drugbank/group
  • experimental (en)
  • illicit (en)
http://linked.open...ugbank/indication
  • Carfentanil is similar (but more potent) to the opioid analgesic fentanyl. It is used as a tranquilizer for large animals. (en)
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Title
  • Carfentanil (en)
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http://linked.open...mechanismOfAction
  • Carfentanil binds very strongly to mu opioid receptors and acts as a competitive agonist. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability. (en)
http://linked.open...ynthesisReference
  • Louis P. Reiff, Paul B. Sollman, "Process of making carfentanil and related analgesics." U.S. Patent US5106983, issued January, 1981. (en)
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  • 59708-52-0 (en)
http://linked.open...k/Bioavailability
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