The voltage-sensing phosphatase (VSP) is the first example of an enzyme controlled by changes in membrane potential. VSP has four distinct regions: the transmembrane voltage-sensing domain (VSD), the inter-domain linker, the cytosolic catalytic domain, and the C2 domain. The VSD transmits the changes in membrane potential through the inter-domain linker activating the catalytic domain which the...

Two chemical probes (4, 5) for the agonist binding sites of serotonin 5-HT2A and 5HT2C receptors were designed as rigid analogs of the methoxylated hallucinogenic phenylalkylamines. These drugs, hybrids of previously constructed heterocycles, include 5and 6-membered oxygen-containing rings that restrict the conformational freedom of the alkoxy ring substituents. Various strategies were explored...

While the endogenous fatty acid amide oleamide has hypnotic properties, neither the breadth of its behavioral actions nor the mechanism(s) by which these behaviors may be mediated has been elucidated. Therefore, the effects of oleamide on the performance of rats in tests of motor function, analgesia, and anxiety were investigated. Oleamide reduced the distance traveled in the open field (ED50 =...

Expression of G protein alpha subunits of the Gq family with various G protein-coupled receptors induces activation of an inositol 1,4, 5-trisphosphate (IP3)/Ca2+-mediated Cl- conductance in Xenopus oocytes. Our present data show that two members of this family, the human Galpha16 subunit and the murine homologue Galpha15, can induce both activation and inhibition of these agonist-induced curre...

The protein Discovered On Gastrointestinal stromal tumors (GIST) protein 1 (DOG1) is a biomarker used in the diagnosis of this type of neoplasm. Nevertheless, high DOG1 expression levels cannot only be detected in GIST, but also in a considerable number of other tumors [1]. DOG1 is also known as ANOctamin 1 (ANO1) and TransMEMbrane protein with unknown function 16A (TMEM16A) and belongs to a su...

Serotoninergic fibers densely innervate olfactory bulb glomeruli, the first sites of synaptic integration in the olfactory system. Acting through 5HT2A receptors, serotonin (5HT) directly excites external tufted cells (ETCs), key excitatory glomerular neurons, and depolarizes some mitral cells (MCs), the olfactory bulb's main output neurons. We further investigated 5HT action on MCs and determi...