Lesopitron dihydrochloride is a full and selective5-HT_1Areceptor agonist withIC₅₀of 125 nM in rat hippocampal membranes.

In vitro binding and autoradiographic studies with [³H]8-OH-DPAT and [³H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT_1Areceptors in the rat brain with a relatively high affinity (pK_i=7.35). As expected of a full agonist at postsynaptic 5-HT_1Areceptors, Lesopitron (IC₅₀=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, IC₅₀=120 nM)^[1].

Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID₅₀=35 μg/kg i.v.)^[1]. 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^[2].

393.74

Solid

C₁₅H₂₃Cl₃N₆

132449-89-9

来索吡琼二盐酸盐

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)