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ChemInform Abstract: Probes for Narcotic Receptor Mediated Phenomena. Part 19. Synthesis of (+)-4-((αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)- 3-methoxybenzyl)-N,N-diethylbenzamide (SNC 80): A Highly Selective, Nonpeptide δ Opioid Receptor Agonis

Autor: Peg Davis, Heng Xu, J. L. Flippen-Anderson, E. J. Bilsky, Richard B. Rothman, K. C. Rice, Robert W. McNutt, L.E. Smith, F Porreca, S. N. Calderon

Publikováno v: ChemInform. 25

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2dde6d455aebcec8d3dc382b31d6e0a0
https://doi.org/10.1002/chin.199448177

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Inverse agonists and neutral antagonists at mu opioid receptor (MOR): possible role of basal receptor signaling in narcotic dependence

Autor: D, Wang, K M, Raehal, E J, Bilsky, W, Sadée

Publikováno v: Journal of neurochemistry. 77(6)

The mu opioid receptor, MOR, displays spontaneous agonist-independent (basal) G protein coupling in vitro. To determine whether basal MOR signaling contributes to narcotic dependence, antagonists were tested for intrinsic effects on basal MOR signali

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::1825e0059b5545f109ec7786a9556db5
https://pubmed.ncbi.nlm.nih.gov/11413242

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Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid receptor ligands

Autor: S N, Calderon, K C, Rice, R B, Rothman, F, Porreca, J L, Flippen-Anderson, H, Kayakiri, H, Xu, K, Becketts, L E, Smith, E J, Bilsky, P, Davis, R, Horvath

Publikováno v: Journal of medicinal chemistry. 40(5)

The highly selective delta (delta) opioid receptor agonist SNC 80 [(+)-4- [(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N ,N- diethylbenzamide, (+)-21] and novel optically pure derivatives were synthesized from the en

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::cb9fab9673e81ff0554c8c32bf44bd08
https://pubmed.ncbi.nlm.nih.gov/9057856

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Treatment with antisense oligodeoxynucleotide to a conserved sequence of opioid receptors inhibits antinociceptive effects of delta subtype selective ligands

Autor: Josephine Lai, E. J. Bilsky, F. Porreca

Publikováno v: Journal of receptor and signal transduction research. 15(1-4)

Previous work has suggested the existence of subtypes of the delta opioid receptor (DOR) which have been termed delta1 and delta2. [D-Ala2, Glu4]deltorphin has been suggested to selectively elicit antinociception via the delta2 receptor while [D-Pen2

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2b9a1c56af56385be15e0aa582c4f64
https://pubmed.ncbi.nlm.nih.gov/8903970

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Constitutive mu opioid receptor activation as a regulatory mechanism underlying narcotic tolerance and dependence

Autor: Z, Wang, E J, Bilsky, F, Porreca, W, Sadée

Publikováno v: Life sciences. 54(20)

Chronic administration of narcotic mu opioid agonists results in tolerance and dependence. We propose that agonist stimulation causes a gradual conversion of mu receptors to a constitutively active state (mu*) as a key step in tolerance and physical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::6fd1b4503858458e89ce9ac18713764b
https://pubmed.ncbi.nlm.nih.gov/7514710

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