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001-es BibID:	BIBFORM102090
035-os BibID:	(Wos)000795409200001 (Scopus)85129843955
Első szerző:	Marton János
Cím:	Diels-Alder Adducts of Morphinan-6,8-Dienes and Their Transformations / Marton János, Fekete Anikó, Cumming Paul, Hosztafi Sándor, Mikecz Pál, Henriksen Gjermund
Dátum:	2022
ISSN:	1420-3049
Megjegyzések:	6,14-ethenomorphinans are semisynthetic opiate derivatives containing an ethylene bridge between positions 6 and 14 in ring-C of the morphine skeleton that imparts a rigid molecular structure. These compounds represent an important family of opioid receptor ligands in which the 6,14-etheno bridged structural motif originates from a [4 + 2] cycloaddition of morphinan-6,8-dienes with dienophiles. Certain 6,14-ethenomorphinans having extremely high affinity for opioid receptors are often non-selective for opioid receptor subtypes, but this view is now undergoing some revision. The agonist 20R-etorphine and 20R-dihydroetorphine are several thousand times more potent analgesics than morphine, whereas diprenorphine is a high-affinity non-selective antagonist. The partial agonist buprenorphine is used as an analgesic in the management of post-operative pain or in substitution therapy for opiate addiction, sometimes in combination with the non-selective antagonist naloxone. In the context of the current opioid crisis, we communicated a summary of several decades of work toward generating opioid analgesics with lesser side effects or abuse potential. Our summary placed a focus on Diels-Alder reactions of morphinan-6,8-dienes and subsequent transformations of the cycloadducts. We also summarized the pharmacological aspects of radiolabeled 6,14-ethenomorphinans used in molecular imaging of opioid receptors.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Molecules. - 27 : 9 (2022), p. 1-111. -
További szerzők:	Fekete Anikó (1973-) (vegyész) Cumming, Paul Hosztafi Sándor Mikecz Pál (1956-) (vegyész) Henriksen, Gjermund
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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