Showing papers in "Neuropharmacology in 1996"

TL;DR: The recent characterization of D3 and D4 receptors which are, interestingly, expressed in areas of the CNS mediating cognition and affect or showing increased affinity for certain neuroleptics, have renewed the interest and hope of finding effective neurolePTics devoid of side effects.

TL;DR: Novel families of potassium channel genes were revealed, as well as conserved homologues of all known vertebrate families, and an exceptionally large class of at least 23 genes with a novel subunit structure having two tandem 'P' domains are revealed.

TL;DR: These results suggested that paxilline blocked maxi-K channels at a site distance from the ChTX binding site located near the external entrance to the pore, suggesting an allosteric interaction between calcium and pxilline.

TL;DR: It is shown that brain penetration is essential for the anti-emetic action of systemically administered NK1 receptor antagonists with and without brain penetration to central NK1 receptors sites.

TL;DR: It is reported that one commonly used, charged reagent (MTSEA; aminoethyl methanethiosulfonate) can cross the membrane quite readily and that other reagents that are quite membrane-impermeant canCross the membrane when patches are electrically leaky, arguing for caution in the use of modifying reagents to determine the membrane topology of channels and other membrane proteins.

TL;DR: Results indicate that 2,3-benzodiazepines are potent, selective and stereospecific antagonists of the AMPA subtype of the non-NMDA glutamate receptor.

TL;DR: A new polyclonal antipeptide antiserum was developed to the γ2 subunit and used in high resolution, postembedding, immunoelectron-microscopic procedures to determine the location of channels containing the ν subunit in relation to GABA-releasing terminals on the surface of neurons.

TL;DR: It is concluded that [3H]L-655,708 is the first radioligand to date which is selective for any BZ2 subtype of the GABAA receptor and should provide a valuable tool for elucidating the structure and function of the alpha 5-containing GabAA receptor subtype.

TL;DR: Heterologous coexpression of either sap97 or PSD-95 with various Shaker-type subunits results in the coclustering of these proteins with the K+ channels, which results in large round intracellular aggregates into which both SAP97 and the K+, channel proteins are colocalized.

TL;DR: It is concluded that neuroactive steroids are highly effective in protecting against pilocarpine- and kainic acid-induced seizures and status epilepticus in mice, and may be of utility in the treatment of some forms of status epileptus in humans.

TL;DR: CPPG is the most potent antagonist yet described for both L-AP4- and (1S,3S)-ACPD-sensitive presynaptic mGlu receptors but displays a 30-fold selectivity for the L- AP4-sensitive receptor over the ( 1S,2-amino-4-phosphonobutyrate-1,3-dicarboxylic acid) receptor.

TL;DR: In immunopurified receptors, the gamma-subunit variants were found to be assembled with different variants of alpha- and beta-subunits, indicating that not only the gamma 2-sub unit gamma 1- and gamma 3-sub units are part of various receptor subtypes.

TL;DR: 5-HT2A antagonists may be effective peripherally acting analgesics or analgesic adjuncts in pain associated with 5-HT release from platelets, such acute injury and, perhaps, some chronic pain states.

TL;DR: A-85380 displays a profile of robust activation of a number of nAChR subtypes with substantially less affinity for [ 125 I]α-BgT sites than [ 3 H](-)-cytisine sites, suggesting that it may serve as a more selective pharmacologic probe for the αx4β2 subtype relative to the α7 and α1β1δg nA ChRs than (±)-epibatidine.

TL;DR: The cerebellum is an ideal vertebrate brain region for investigating issues concerning GABAA receptors and the functions of the different subtypes.

TL;DR: It is reported that anandamide directly inhibits (IC50, 2.7 muM) Shaker-related Kv1.2 K+ channels that are found ubiquitously in the mammalian brain.

TL;DR: The results suggest that distinct subunit composition confers specific deactivation and desensitization properties that may profoundly affect synaptic decay kinetics and the capability to sustain high frequency synaptic inputs.

TL;DR: The effects of repeated administration of both antidepressant drugs with a range of pharmacological actions and of electroconvulsive shock on noradrenaline reuptake sites were examined and data support the view that [3H]nisoxetine binds to a single population of homogeneous sites associated with the nor adrenaline transporter complex.

TL;DR: Clozapine exhibited 10-fold higher affinity than haloperidol for human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT 1A) and the stimulation was antagonized by the selective 5- HT1A receptor antagonist, WAY 100635.

TL;DR: Results provide the first direct physiological evidence for pharmacological modulation of microscopic binding affinity of GABA receptors and indicate that diazepam likely enhances GABA receptor currents primarily by accelerating GABA association to its receptor at the first agonist binding site.

TL;DR: Basic properties of Eag and M-EAG channels expressed in frog oocytes are described, using two-electrode voltage clamp and patch clamp techniques, and no evidence for Ca2+ flux through Eag channels is found.

TL;DR: The generation and characterization of monoclonal antibodies against eight distinct mammalian K + channel polypeptides and the subtype-specificity of these mAbs against native K + channels in mammalian brain and against recombinant K +annels expressed in transfected mammalian cells are characterized.

TL;DR: The results are consistent with a model of diazepam dependence based on GABAA receptor subunit isoform switching and changes in the levels of mRNAs arising from a given gene cluster was noted.

TL;DR: In mice and rats, both enantiomers revealed a similar neuroprotective potency when they were administered subcutaneously 1 or 2 hr before occlusion of the middle cerebral artery (MCA), whereas a longer time period of pretreatment failed to exert neuroprotection.

TL;DR: The phosphoinositide response in the rat hippocampus to 1S,3R-ACPD is mediated by a synergistic interaction between group 1 and group 2 mGlu receptors, and is found to greatly enhance phosphoinposide hydrolysis to DHPG or quisqualate.

TL;DR: The similarity of the pKBs reported in this study to those previously reported using native neuronal preparations, which are likely to represent heterogeneous GABAA receptor populations, further indicates the lack of dependence on receptor subunit composition for the inhibitory action of bicuculline.

TL;DR: Anti-nociceptive effects of neuronal nicotinic acetylcholine receptor (NAChR) ligands were evaluated and indicated that a sub-population of NAChR receptors are located pre-synaptically on noradrenergic and/or serotoninergic pathways in the hippocampus, indicating a minimal role for these receptors in the tail-flick response.

TL;DR: The ability of PREG-S to block retention performance deficits as well as motor impairment induced by D-AP5 is in agreement with its positive modulatory action at NMDA receptors.

TL;DR: DHA may serve as a local messenger molecule that selectively modulates the activity of certain voltage-gated K+ channels in a Zn2(+)-dependent fashion.

TL;DR: E2020, which inhibits brain ChE by a novel, reversible mechanism, elevates extracellular ACh in a comparable manner to other centrally-active ChEI, and this elevation of ACh is associated with stimulation of catecholamine release.