Nagase Hiroshi

Pertussis toxin abolishes μ- and δ-opioid agonist-induced place perference

Abstract The effects of i.c.v. treatment with pertussis toxin (PTX) on the motivational effect of opioid agonists were examined in mice Morphine (0.1–10 nmol, i.c.v.). [D-Ala 2 , N-MePhe 4 . Gly-ol 5 ]enkephalin (DAGO. 0.001–0.1 nmol, i.c.v.). a sclective μ-opioid receptor agonist, and [D-Pen 2 , D-Pen 2 ]enkephalin (DPDPE, 1–15 nmol. i.c.v. a selective δ-opioid receptor agonist, produced a dose-related place preference in mice. Administration of PTX (0.5 μg. i.c.v.) to mice resulted in no preference for either the drug- or vehicle-associated place. Pretreatment with PTX abolished the place preferences induced by DAGO (0.1 nmol). morphine (10 nmol) and DPDPE (15 nmol). These findings demonstrate that the appetitive effects of opioids result from the activation of central μ- and δ-receptors. and suggest that PTX-sensitive GTP-bindtng proteins in the central nervous system may be involved in the motivational effects of μ- and δ-opioid agonists.

Synthesis of (+)-5,6,7-trinor-4,8-inter-m-phenylene PGI2

Abstract The titled compound, which is a stable and potent analog of prostacyclin, was synthesized from readily available 1,4-dibromocyclopentene via cyclopenta[b]benzofuran carboxylic acid 5 .