Reference of 93-17-4, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 93-17-4, Name is 3,4-Dimethoxyphenylacetonitrile, SMILES is C1=C(CC#N)C=CC(=C1OC)OC, belongs to isothiazole compound. In a article, author is DOBLE, A, introduce new discover of the category.
PHARMACOLOGICAL CHARACTERIZATION OF RP-62203, A NOVEL 5-HYDROXYTRYPTAMINE 5-HT2 RECEPTOR ANTAGONIST
1 RP 62203 (2-[3-(4-(4-fluorophenyl)-piperazinyl)propyl]naphto[1,8-ca]isothiazole-1,1-dioxide) is a novel naphtosultam derivative which shows very high affinity for 5-HT2 receptors in the rat cerebral cortex (K(i) = 50.0 pM). 2 RP 62203 is relatively selective for this sub-type of 5-hydroxytryptamine (5-HT) receptor, having lower affinity for the 5-HT1A receptor and very low affinity for the 5-HT3 receptor. RP 62203 displayed low to moderate affinity for alpha(1)-adrenoceptors, dopamine D2 receptors and histamine H-1 receptors. 3 In vivo binding experiments demonstrated that oral administration of low doses of RP 62203 led to a long-lasting (> 6 h) occupation of cortical 5-HT2 receptors (ID50 = 0.39 mg kg-1). 4 In cortical slices from the neonatal rat, RP 62203 potently inhibited inositol phosphate formation evoked by 5-HT, with an IC50 of 7.76 nM. 5 The activity of neurones in the raphe and their responses to microiontophoretically applied 5-HT were studied with extracellular recording electrodes in the anaesthetized rat. RP 62203 potently and dose-dependently blocked excitations evoked by 5-HT when administered at doses of 0.5-4.0 mg kg-1, i.p. In contrast, neither 5-HT-evoked depressions nor glutamate-evoked excitations of raphe neuronal firing were blocked by RP 62203 at doses as high as 8.0 mg kg-1, i.p. 6 Head twitches induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) could be abolished by low doses of RP 62203 in mice (ED50 = 0.44 mg kg-1, p.o.) and in rats (ED50 = 1.54 p.o.). Similar results were obtained with mescaline and 5-hydroxytryptophan (5-HTP). 7 The potency of RP 62203 was compared with that of three other 5-HT2 receptor antagonists, ritanserin, ICI 169,369 and ICI 170,809. In all models, RP 62203 showed similar activity to ritanserin, whilst either ICI 169,369 or ICI 170,809 was several fold less active. 8 It is concluded that RP 62203 is a potent and selective antagonist at 5-HT2 receptors in the rodent central nervous system.
Reference of 93-17-4, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 93-17-4 is helpful to your research.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com