BMC pharmacology
-
Gamma-aminobutyric acid type A (GABAA) receptors provide the main inhibitory control in the brain. Their heterogeneity may make it possible to precisely target drug effects to selected neuronal populations. In situ hybridization using rat brain sections has revealed a unique expression of GABAA receptor epsilon and theta subunit transcripts in the locus coeruleus, where they are accompanied at least by alpha3, alpha2, beta1 and beta3 subunits. Here, we studied the pharmacology of the human alpha3beta1, alpha3beta1epsilon, alpha3beta1theta and alpha3beta1epsilontheta receptor subtypes expressed in Xenopus oocytes and compared them with the gamma2 subunit-containing receptors. ⋯ The epsilon and theta subunits bring additional features to alpha3beta1 GABAA receptors. These receptor subtypes may constitute as novel drug targets in selected brain regions, e.g., in the brainstem locus coeruleus nuclei.
-
6-Shogaol is one of the major compounds in the ginger rhizome that may contribute to its anti-inflammatory properties. Confirmation of this contribution was sought in this study in Sprague- Dawley rats (200-250 g) treated with a single injection (0.5 ml of 1 mg/ml) of a commercial preparation of complete Freund's Adjuvant (CFA) to induce monoarthritis in the right knee over a period of 28 days. During this development of arthritis, each rat received a daily oral dose of either peanut oil (0.2 ml-control) or 6-shogaol (6.2 mg/Kg in 0.2 ml peanut oil). ⋯ From these results, it is concluded that 6-shogaol reduced the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats.