Lesopitron dihydrochloride

Lesopitron dihydrochloride is a full and selective 5-HT 1A receptor agonist with IC 50 of 125 nM in rat hippocampal membranes.In VitroIn vitro binding and autoradiographic studies with [ 3 H]8-OH-DPAT and [ 3 H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT 1A receptors in the rat brain with a relatively high affinity (pK i =7.35). As expected of a full agonist at postsynaptic 5-HT 1A receptors, Lesopitron (IC 50 =125 nM) inhibits forskolin-stimulated adenylate cyclase activity in rat hippocampal membranes to the same extent as 5-HT. Lesopitron inhibits the firing of serotoninergic neurons both in vitro (in brainstem slices, IC 50 =120 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoLesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID 50 =35 μg/kg i.v.) . Lesopitron administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, i.p.) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal administrationRats Male Wistar rats weighing 270-300 g, are used. Lesopitron is administered either through the dialysis probe (dissolved in artificial CSF) or i.p. (dissolved in 0.9% saline, 2 mL/kg body weight). aladdin has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:5-HT 1A Receptor 125 nM (IC 50 , in rat hippocampal membranes). Specification: 0.96 Molecular Formula: C15H23Cl3N6 Molecular Weight: 393.74 PubChem CID: 60812 Isomeric SMILES: C1CN(CCN1CCCCN2C=C(C=N2)Cl)C3=NC=CC=N3.Cl.Cl