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BW373U86

Opioid analgesic drug used in research


Opioid analgesic drug used in research

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(+)-BW373U86 is an opioid analgesic drug used in scientific research.

BW373U86 is a selective agonist for the δ-opioid receptor, with approximately 15× stronger affinity for the δ-opioid than the μ-opioid receptor. It has potent analgesic and antidepressant effects in animal studies. 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.

CNS review:

References

References

  1. (February 1997). "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.
  2. (March 2001). "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.
  3. (November 1993). "A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.". The Journal of Pharmacology and Experimental Therapeutics.
  4. (November 2002). "Comparison of Receptor Mechanisms and Efficacy Requirements for δ-Agonist-Induced Convulsive Activity and Antinociception in Mice". Journal of Pharmacology and Experimental Therapeutics.
  5. (June 2002). "Nonpeptidic δ-opioid Receptor Agonists Reduce Immobility in the Forced Swim Assay in Rats". Neuropsychopharmacology.
  6. (August 2001). "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.
  7. (May 2004). "COX-2 and iNOS in opioid-induced delayed cardioprotection in the intact rat". Life Sciences.
  8. (July 2007). "GSK inhibition and KATP channel opening mediate acute opioid-induced cardioprotection at reperfusion". Basic Research in Cardiology.
  9. (March 1996). "BW373U86: A Non-Peptidic, Systemically-Active δ Opioid Agonist". CNS Drug Reviews.
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