中文名 | lesopitron |
英文名 | lesopitron |
别名 | 来索吡琼二盐酸盐 化合物 T11839 |
英文别名 | E4424 lesopitron Lesopitron (dihydrochloride) |
CAS | 132449-89-9 |
化学式 | C15H22Cl2N6 |
分子量 | 357.28 |
熔点 | 194-197.5° |
存储条件 | Room Temprature |
体外研究 | In 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). |
体内研究 | Lesopitron 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. |
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