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Pathway Description
Propranolol B2-Adrenergic Vasoconstriction Action Pathway
Homo sapiens
Drug Action Pathway
On the World Health Organization's List of Essential Medicines and a prototypical drug of its class, propranolol is a non-cardioselective beta blocker and it is typically synthesized as a racemic mixture of 2 enantiomers where the S(-)-enantiomer has approximately 100 times the binding affinity for beta adrenergic receptors. It can be administered intravenously to the bloodstream or orally, where it passes through hepatic portal circulation, and enters the bloodstream to act on peripheral cells. Propranolol is a non-selective beta adrenergic antagonist used to treat hypertension, angina, atrial fibrillation, myocardial infarction, migraine, essential tremor, hypertrophic subaortic stenosis, and pheochromocytoma. It can be found under the brand names Hemangeol, Hemangiol, Inderal, and Innopran. Propranolol causes vasoconstriction via blockage or antagonism of the beta-2 adrenergic receptors. By blocking these receptors, the G protein signalling cascade is unable to occur, leading to increased levels of intracellular calcium which can then readily bind to calmodulin causing smooth muscle contraction (vasoconstriction in this case). Some side effects of using propranolol may include dizziness, tiredness, and difficulties sleeping.
References
Propranolol B2-Adrenergic Vasoconstriction 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.
Pubmed: 29126136
Hagen R, Ghareeb E, Jalali O, Zinn Z: Infantile hemangiomas: what have we learned from propranolol? Curr Opin Pediatr. 2018 Aug;30(4):499-504. doi: 10.1097/MOP.0000000000000650.
Pubmed: 29846253
Khouri C, Jouve T, Blaise S, Carpentier P, Cracowski JL, Roustit M: Peripheral vasoconstriction induced by beta-adrenoceptor blockers: a systematic review and a network meta-analysis. Br J Clin Pharmacol. 2016 Aug;82(2):549-60. doi: 10.1111/bcp.12980. Epub 2016 May 31.
Pubmed: 27085011
Billington CK, Penn RB: Signaling and regulation of G protein-coupled receptors in airway smooth muscle. Respir Res. 2003;4(1):2. Epub 2003 Mar 14.
Pubmed: 12648290
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