The title mefloquine derivative has been crystallized as its 1:1 methanol solvate, C(19)H(18)F(6)N(2)O(2)·CH(3)OH. Each of the meth-ine-hydroxyl residue [the C-C-C-O torsion angle is -16.35 (17) °] and the piperidinyl group [distorted chair conformation] lies to one side of the quinolinyl ring system. The hydroxyl and carbonyl groups lie to either side of the mol-ecule, enabling their participa...

The present studies were conducted to test the hypothesis that activation of peripheral cannabinoid CB(2) receptors would suppress hyperalgesia evoked by intradermal administration of capsaicin, the pungent ingredient in hot chili peppers. The CB(2)-selective cannabinoid agonist (2-iodo-5-nitro-phenyl)-[1-(1-methyl-piperidin-2-ylmethyl)-1H-indol-3-yl]-methanone (AM1241) (33, 330 microg/kg i.p.)...

Activation of brain nociceptin/orphanin FQ (NOP) receptors leads to attenuation of mu-opioid receptor (MOP receptor)-mediated antinociception. Buprenorphine, a high-affinity partial MOP receptor agonist also binds to NOP receptors with 80 nM affinity. The buprenorphine-induced inverted U-shaped dose-response curve for antinociception may be due to NOP receptor activation, given that, in the pre...

A novel compound 2-(2-ethoxyphenyl)-5-hydroxy-1-(2-hydroxyethyl)-5-methyl piperidin-4-one (II) has been synthesized by a previously well-known reaction between (E)-3-(2-ethoxyphenyl)-1-(2-methyloxiran-2-yl)prop-2-en-1-one (I) and ethanol amine. The was used to synthesize (Z)-2-((2S,5S)-2-(2-ethoxyphenyl)-5-hydroxy-1-(2-hydroxyethyl)-5-methylpiperidin-4-ylidene)hydrazine-1-carbothioamide (III) t...

The purpose of the study was to compare the binding energy of pharmacophores of different classes targeting to kappa opioid receptor (KOR) with ketazocine and pentazocine which are having good activity on the KOR. The 3D structure of KOR receptor was built by Homology modeling; pharmacophores were characterized by using Ligand scout. Docking studies for the KOR agonists were performed in Autodo...

The purpose of the study was to compare the binding energy of pharmacophores of different classes targeting to kappa opioid receptor (KOR) with ketazocine and pentazocine which are having good activity on the KOR. The 3D structure of KOR receptor was built by Homology modeling; pharmacophores were characterized by using Ligand scout. Docking studies for the KOR agonists were performed in Autodo...

Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands...