Abstract
Methods The chemistry involved the design and synthesis of two sets of oxazolomorphinans having the new heteroring anellated to the A-ring of the morphinan backbone. Binding affinities of the newly synthesized compounds at opioid receptors were determined by in vitro competition binding assays using rat brain (μ, δ) and guinea pig brain ( ) membranes and employing [H]DAMGO (μ), [H] [Ile]deltorphin II (δ) and [H]U-69,593 ( ) as specific opioid radioligands. The in vitro pharmacological activities were established using [S]GTPgS functional assays in membranes from Chinese hamster ovary (CHO) cells expressing human opioid receptors.
Highlights
The need for opioid analgesics with reduced undesirable side-effects has initiated a vast amount of scientific efforts, which have led to a number of new opioid ligands and significant expansion of knowledge in opioid pharmacology
The chemistry involved the design and synthesis of two sets of oxazolomorphinans having the new heteroring anellated to the A-ring of the morphinan backbone
Binding studies on the newly synthesized N-methyl and N-allyl derivatives to opioid receptors revealed remarkable results for three compounds: the aminosubstituted N-methyloxazolomorphinan showed high affinity and selectivity to the μ opioid receptor, while two N-allyloxazolomorphinans were found to interact with high affinity with μ and sites and moderate binding towards δ receptors
Summary
The need for opioid analgesics with reduced undesirable side-effects has initiated a vast amount of scientific efforts, which have led to a number of new opioid ligands and significant expansion of knowledge in opioid pharmacology. Development of novel N-methyl and N-allylsubstituted oxazolomorphinans and their interaction with opioid receptors Attila Sipos1,2*, Levente Girán1, Sándor Berényi1, Sándor Antus1, Helmut Schmidhammer2, Mariana Spetea2
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