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5-HT1A receptors mediate various serotonergic functions and may be implicated in various pathologies including depressive and anxiety disorders, Alzheimer’s disease, and schizophrenia. WAY-100635 is a potential SPECT ligands for the 5-HT1A receptor.

In vitro: WAY-100635 displaced specific binding of the 5-HT1A radioligand, [3H]8-OH-DPAT, to rat hippocampal membranes with a plC50 of 8.87. In functional assays, WAY-100635 was a potent 5-HT1A receptor antagonist, with no evidence of any 5-HTIA receptor agonist or partial agonist activity. In the isolated guinea-pig ileum WAY-100635 was a potent and, at high concentrations, an insurmountable antagonist of the 5-HT1A receptor agonist action of 5-carboxamidotryptamine, with an apparent pA 2 value (at 0.3 nM) of 9.71 [2].

In vivo: WAY-100635 blocked the inhibitory action of 8-OH-DPAT on dorsal raphe neuronal firing in the anaesthetised rat at doses which had no inhibitory action per se. In behavioural models, WAY-100635 itself induced no overt behavioural changes but potently antagonised the behavioural syndrome induced by 8-OH-DPAT in the rat and guinea-pig (minimum effective dose = 0.003 mg/kg s.c. and ID50 = 0.01 mg/kg s.c., respectively). WAY-100635 also blocked the hypothermia induced by 8-OH-DPAT in the mouse and rat with ID50 values of 0.01 mg/kg s.c. [2].

Clinical trial: Using the ligand [11C]-WAY100635, an open label, non-randomized positron emission tomography study in healthy male subjects has been conducted to investigate brain 5-HT1A receptor occupancy, pharmacokinetics and safety of single oral doses of GSK163090.

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