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Pathway Description
Carfentanil Opioid Agonist Action Pathway
Homo sapiens
Drug Action Pathway
Carfentanil is an analogue of the popular synthetic opioid analgesic fentanyl, and is one of the most potent opioids known. It is used as a tranquilizer for large animals.
Carfentanil acts primarily on the mu (some kappa and delta) opioid receptors as an agonist. It will induce similar effects of analgesia as other opioids, however, due to its potency, it will also induce strong side effects such as sedation. Consequently, that is why it is used as a tranquilizer for large animals.
Carfentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the brain, spinal cord, and other tissues. It exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Carfentanil also depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
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 GABA is inhibited. 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. Carfentanil acts at A delta and C pain fibres in the dorsal horn of the spinal cord. By decreasing neurotransmitter action there is less pain transmittance into the spinal cord. This leads to less pain perception.
References
Carfentanil Opioid Agonist Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Nassirpour R, Bahima L, Lalive AL, Luscher C, Lujan R, Slesinger PA: Morphine- and CaMKII-dependent enhancement of GIRK channel signaling in hippocampal neurons. J Neurosci. 2010 Oct 6;30(40):13419-30. doi: 10.1523/JNEUROSCI.2966-10.2010.
Pubmed: 20926668
Chan P, Lufty K. Molecular Changes in Opioid Addiction: The Role of Adenylyl Cyclase and cAMP/PKA System. Progress in Molecular Biology and Translational Science, Volume 137: 203-219, 2016.
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