The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mouse models of acute pain and cocaine-induced reward.

Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain.

Nociceptin/orphanin FQ peptide receptor (NOP) agonists produce antinociceptive effects in animal models after spinal administration and potentiate μ-opioid receptor (MOP)-mediated antinociception. This study determined the antinociceptive effects of spinally administered bifunctional NOP/MOP ligands and the antinociceptive functions of spinal NOP and MOP receptors in mice. Antinociceptive effec...

Buprenorphine

In the crystal structure of a semi-synthetic opioid drug buprenorphine, C29H41NO4 {systematic name: (2S)-2-[(5R,6R,7R,14S)-9α-cyclo-propyl-methyl-3-hy-droxy-6-meth-oxy-4,5-ep-oxy-6,14-ethano-morphinan-7-yl]-3,3-di-methyl-butan-2-ol}, the cyclo-propyl-methyl group is disordered over two sites with an occupancy factor of 0.611 (3) for the major component. One of the hy-droxy groups is involved in...

Characterization of the In Vitro Profile and In Vivo Behavioral Effects in Mouse Models of Acute Pain and Cocaine-induced Reward

Comparison of various density functional methods for distinguishing stereoisomers based on computed (1)H or (13)C NMR chemical shifts using diastereomeric penam beta-lactams as a test set.

Full (1)H and (13)C NMR chemical shift assignments were made for two sets of penam beta-lactams: namely, the diastereomeric (2S, 5S, 6S)-, (2S, 5R, 6R)-, (2S, 5S, 6R)-, and (2S, 5R, 6S)-methyl 6-(1,3-dioxoisoindolin-2-yl)-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylates (1-4) and (2S, 5R, 6R)-, (2S, 5S, 6R)-, and (2S, 5R, 6S)-6-(1,3-dioxoisoindolin-2-yl)-3,3-dimethyl-7-oxo-4...

Comparative Effects of LY3020371, a Potent and Selective mGlu2/3 Receptor Antagonist, and Ketamine, a Non-Competitive NMDA Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists for the Treatment of Depression

245 words Tables: 6 Figures: 14 Abbreviations: ACh: acetylcholine; AMPA: -Amino-3-hydroxy-5-methyl-4isoxazolepropionic acid; DHPG: 3,4-Dihydroxyphenylglycine; DOPAC: 3,4Dihydroxyphenylacetic acid; GABA: gamma aminobutyric acid; 5-HT: 5-hydroxytryptamine or serotonin; 5-HIAA: 5-hydroxyindolacetic acid; LY341495: (2S)-2-amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid; mGl...