Chemistry:BW-501C67

From HandWiki

BW-501C67 is a peripherally selective serotonin 5-HT2A and 5-HT2C receptor antagonist which is used in scientific research.[1][2][3][4][5][6] It shows selectivity for the serotonin 5-HT2 receptors over the α1-adrenergic receptor.[1]

The drug antagonizes peripheral but not central effects of serotonin receptor agonists like serotonin.[2][3][7][6] As examples, it has been found to antagonize the sympathomimetic effects of serotonin in animals, including vasoconstriction and pressor effects, but does not block centrally mediated effects like increased corticosterone secretion or myoclonus.[3][7][8][6]

BW-501C67 and analogues were patented for use in combination with serotonin 5-HT2A receptor agonists like serotonergic psychedelics in 2023.[9]

See also

References

  1. ↑ 1.0 1.1 "Chapter 5. Drugs Acting at Central 5-Hydroxytryptamine Receptors". Annual Reports in Medicinal Chemistry. 21. Elsevier. 1986. pp. 41–50. doi:10.1016/s0065-7743(08)61115-x. ISBN 978-0-12-040521-3. 
  2. ↑ 2.0 2.1 "Important messages in the 'post': recent discoveries in 5-HT neurone feedback control". Trends in Pharmacological Sciences 28 (12): 629–636. December 2007. doi:10.1016/j.tips.2007.10.009. PMID 17996955. 
  3. ↑ 3.0 3.1 3.2 "5-HT-mediated behavior. Animal studies". Neuropharmacology 23 (12B): 1521–1528. December 1984. doi:10.1016/0028-3908(84)90096-0. PMID 6152026. 
  4. ↑ "Central cardiovascular regulation and 5-hydroxytryptamine receptors". Brain Research Bulletin 56 (5): 425–439. November 2001. doi:10.1016/s0361-9230(01)00612-8. PMID 11750788. 
  5. ↑ "5-HT1C/5-HT2 receptor blockade prevents 1-(2,5-dimethoxy-4-iodophenyl)2-aminopropane-, but not stress-induced increases in brain tryptophan". European Journal of Pharmacology 231 (1): 77–82. January 1993. doi:10.1016/0014-2999(93)90686-c. PMID 8095238. 
  6. ↑ 6.0 6.1 6.2 "Antagonism of a peripheral vascular but not an apparently central serotonergic response by xylamidine and BW 501C67". European Journal of Pharmacology 125 (1): 71–77. June 1986. doi:10.1016/0014-2999(86)90084-1. PMID 3732393. 
  7. ↑ 7.0 7.1 "The pharmacology of cerebral vasospasm". Pharmacology 29 (1): 1–16. 1984. doi:10.1159/000137986. PMID 6379682. 
  8. ↑ "Serotonin receptors involved in regulation of pituitary-adrenocortical function in rats". Behavioural Brain Research 73 (1–2): 215–219. 1996. doi:10.1016/0166-4328(96)00099-x. PMID 8788505. 
  9. ↑ Kruegel AC, "Combinations of peripheral 5-HT2A receptor antagonists and central 5-HT2A receptor agonists", WO patent 2023028086, published 2 March 2023




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