Dantrolene inhibits and ryanodine stimulates calcium release from skeletal-muscle sarcoplasmic reticulum (SR), the former by an unknown mechanism, and the latter by activating the ryanodine receptor (RyR), the primary Ca2+-release channel of SR. Dantrolene is used to treat malignant hyperthermia (MH), a genetic predisposition to excessive intracellular Ca2+ release upon exposure to volatile ana...

Previous studies have demonstrated that when tritiated proline [( 3H]Pro) is injected into the dorsal column nuclei (DCN) of cats, it labels macroglial cells, but fails to label neurons at the injection site. (Tritiated leucine [( 3H]Leu) in contrast, labels both neurons and some glial cells.) Despite the failure of [3H]Pro to label DCN neurons, labeling is still observed in DCN terminal target...

In this study, theophylline (1) compounds were synthesized with addition of 2-bromoetha-nol, 2-bromoacetamide and methyl-2-bromoacetate to attain symmetric connections NHCs (2a–c). New complexes containing the N-heterocyclic carbene (NHC) ligands using azolium salts in dimethyl formamide (DMF). After NHC predecessor reacted Ag2O, Ag(I)-NHC following: 7,9-di-(2-hydroxyethyl)-8,9-dihydro-1,3-dime...

• GPR120 (short isoform) homology model used for docking-based virtual screening (DBVS) of ligand database. Combination approach in silico and vitro to discover potential anti-cancer compounds targeting GPR120. Identification a dihydrospiro(benzo[ h ]quinazoline-5,1?-cyclopentane)-4(3H)-one scaffold activity. The G-protein coupled receptor - has recently been implicated as novel target colorect...

an efficient three-component reaction of dialkyl acetylendicarboxylates and 2-pyrrolidin in the presence of triphenylphosphine produces dialkyl 2-(2-pyrrolidin-n-yl)-3-(triphenylphosphanylidene)succinate. these phosphoranes undergo mild intramolecular wittig reaction to produce dialkyl (e)-2-(4,5-dihydro-3h-pyrrol-2-yl)fumarate in excellent yields.

We have developed an array of assays for nicotinic acetylcholine receptor binding and function. [125I]alpha-Bungarotoxin-, (-)-[3H]nicotine-, and [3H]epibatidine-binding nicotinic acetylcholine receptors were assayed in mouse brain membranes and sections. Nicotinic acetylcholine receptor function was quantified using synaptosomal [3H]dopamine, [3H]gamma-aminobutyric acid ([3H]GABA), and 86Rb(+)...

The importance of the lateral habenula-dorsal raphe pathway in the control of in vivo [3H]serotonin release in the cat basal ganglia was examined using the push-pull cannula technique and an isotopic method for the estimation of [3H]serotonin continuously formed from [3H]tryptophan. [3H]Serotonin was measured in both caudate nuclei and substantiae nigra and, in some cases, in the dorsal raphe. ...

The [3H]leukotriene C4 ([3H]LTC4) and [3H]leukotriene D4 ([3H] LTD4) specific binding sites in guinea-pig lung membranes were characterized and correlated with smooth muscle contractile activities of a series of LTC-, D- and E-type analogs. [3H]LTC4 bound to the specific sites with high affinity (dissociation constant Kd = 15 +/- 5 nM), saturable capacity (maximum binding = 68 +/- 15 pmol/mg of...