Chemistry:BW373U86
From HandWiki
Short description: Opioid analgesic drug used in research
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| Other names | (+)-BW373U86 |
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| Formula | C27H37N3O2 |
| Molar mass | 435.612 g·mol−1 |
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(+)-BW373U86 is an opioid analgesic drug used in scientific research.[1][2]
BW373U86 is a selective agonist for the δ-opioid receptor, with approximately 15× stronger affinity for the δ-opioid than the μ-opioid receptor.[3] It has potent analgesic and antidepressant effects in animal studies.[4][5] In studies on rats, BW373U86 appears to protect heart muscle cells from apoptosis in conditions of ischemia (oxygen deprivation, such as in heart attack). The mechanism for this is complex and may be separate from its delta agonist effects.[6][7][8]
References
- ↑ "Probes for Narcotic Receptor Mediated Phenomena. 23.1 Synthesis, Opioid Receptor Binding, and Bioassay of the Highly Selective δ Agonist (+)-4-[(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and Related Novel Nonpeptide δ Opioid Receptor Ligands". Journal of Medicinal Chemistry 40 (5): 695–704. February 1997. doi:10.1021/jm960319n. PMID 9057856.
- ↑ "Factors Influencing Agonist Potency and Selectivity for the Opioid δ Receptor Are Revealed in Structure−Activity Relationship Studies of the 4-[(N-Substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides". Journal of Medicinal Chemistry 44 (6): 972–987. March 2001. doi:10.1021/jm000427g. PMID 11300879.
- ↑ "A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.". The Journal of Pharmacology and Experimental Therapeutics 267 (2): 852–857. November 1993. PMID 8246159. http://jpet.aspetjournals.org/content/267/2/852.abstract.
- ↑ "Comparison of Receptor Mechanisms and Efficacy Requirements for δ-Agonist-Induced Convulsive Activity and Antinociception in Mice". Journal of Pharmacology and Experimental Therapeutics 303 (2): 723–729. November 2002. doi:10.1124/jpet.102.036525. PMID 12388657.
- ↑ "Nonpeptidic δ-opioid Receptor Agonists Reduce Immobility in the Forced Swim Assay in Rats". Neuropsychopharmacology 26 (6): 744–755. June 2002. doi:10.1016/S0893-133X(01)00413-4. PMID 12007745.
- ↑ "BW373U86, a δ Opioid Agonist, Partially Mediates Delayed Cardioprotection via a Free Radical Mechanism that is Independent of Opioid Receptor Stimulation". Journal of Molecular and Cellular Cardiology 33 (8): 1455–1465. August 2001. doi:10.1006/jmcc.2001.1408. PMID 11448134.
- ↑ "COX-2 and iNOS in opioid-induced delayed cardioprotection in the intact rat". Life Sciences 75 (2): 129–140. May 2004. doi:10.1016/j.lfs.2003.10.036. PMID 15120566.
- ↑ "GSK3β inhibition and KATP channel opening mediate acute opioid-induced cardioprotection at reperfusion". Basic Research in Cardiology 102 (4): 341–349. July 2007. doi:10.1007/s00395-007-0651-6. PMID 17450314.
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