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1531-12-0Relevant articles and documents
Preliminary pharmacological evaluation of enantiomeric morphinans
Sromek, Anna W.,Provencher, Brian A.,Russell, Shayla,Chartoff, Elena,Knapp, Brian I.,Bidlack, Jean M.,Neumeyer, John L.
, p. 93 - 99 (2014/03/21)
A series of levo- and dextromorphinan pairs have been synthesized and evaluated for their affinities to the mu, kappa, and delta opioid receptors, the N-methyl-d-aspartate (NMDA) channel, and sigma 1 and 2 receptors. It was found that levo isomers tended to have higher affinities at the opioid receptors and moderate to high affinities to the NMDA and sigma receptors, while dextro isomers tended to have lower affinities to the opioid receptors but comparatively higher affinities to the NMDA and sigma receptors. This series of compounds have interesting and complex pharmacological profiles, and merit further investigation as potential therapies for drug abuse treatment.
Anticonvulsant effects of new morphinan derivatives
Kim, Hyoung-Chun,Nabeshima, Toshitaka,Jhoo, Wang-Kee,Ko, Kwang Ho,Kim, Won-Ki,Shin, Eun-Joo,Cho, Minkyoung,Lee, Phil Ho
, p. 1651 - 1654 (2007/10/03)
We synthesized a series of compounds that are modified in positions 3 and 17 of the morphinan ring system, with the intention of developing ideal anticonvulsant agents. We examined the effects of these compounds on kainic acid (KA)-induced seizures, and on locomotor patterns in rats. We found that compounds 5, 6, and 8 exhibit novel anticonvulsant effects, with negligible psychotropic effects.
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: Mixed κ agonists and μ agonists/antagonists as potential pharmacotherapeutics for cocaine dependence
Neumeyer, John L.,Bidlack, Jean M.,Zong, Rushi,Bakthavachalam, Venkatesalu,Gao, Peng,Cohen, Dana J.,Negus, S. Stevens,Mello, Nancy K.
, p. 114 - 122 (2007/10/03)
This report concerns the synthesis and preliminary pharmacological evaluation of a novel series of K agonists related to the morphinan (-)- cyclorphan (3a) and the benzomorphan (-)cyclazocine (2) as potential agents for the pharmacotherapy of cocaine abuse. Recent evidence suggests that agonists acting at κ opioid receptors may modulate the activity of dopaminergic neurons and alter the neurochemical and behavioral effects of cocaine. We describe the synthesis and chemical characterization of a series of morphinans 3a-c, structural analogues of cyclorphan [(-)-3-hydroxy-N- cyclopropylmethylmorphinan S(+)-mandelate, 3a], the 10-ketomorphinans 4a,b, and the 8-ketobenzomorphan 1b. Binding experiments demonstrated that the cyclobutyl analogue 3b [(-)-3-hydroxy-N-cyclobutylmethylmorphinan S(+)- mandelate, 3b, MCL-101] of cyclorphan (3a) had a high affinity for μ, δ, and κ opioid receptors in guinea pig brain membranes. Both 3a,b were approximately 2-fold more selective for the κ receptor than for the μ receptor. However 3b (the cyclobutyl analogue) was 18-fold more selective for the κ receptor in comparison to the δ receptor, while cyclorphan (3a) had only 4-fold greater affinity for the κ receptor in comparison to the δ receptor. These findings were confirmed in the antinociceptive tests (tail- flick and acetic acid writhing) in mice, which demonstrated that cyclorphan (3a) produced antinociception that was mediated by the δ receptor while 3b did not produce agonist or antagonist effects at the δ receptor. Both 3a,b had comparable κ agonist properties 3a,b had opposing effects at the μ receptor: 3b was a μ agonist whereas 3a was a μ antagonist.