An atypical antipsychotic
Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM).1,2 It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). Risperidone (0.1 mg/kg per day, i.p.) attenuates deficits in prepulse inhibition of the acoustic startle response, but not deficits in social interaction, in a rat neonatal ventral hippocampal lesion model of schizophrenia.3 Formulations containing risperidone have been used in the treatment of schizophrenia and bipolar disorder.
1.Leysen, J.E., Janssen, P.M., Gommeren, W., et al.In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidoneMol. Pharmacol.41(3)494-508(1992) 2.Bymaster, F.P., Calligaro, D.O., Falcone, J.F., et al.Radioreceptor binding profile of the atypical antipsychotic olanzapineNeuropsychopharmacology14(2)87-96(1996) 3.Rueter, L.E., Ballard, M.E., Gallagher, K.B., et al.Chronic low dose risperidone and clozapine alleviate positive but not negative symptoms in the rat neonatal ventral hippocampal lesion model of schizophreniaPsychopharmacology (Berl.)176(3-4)312-319(2004)
Animal experiment: | Rats[2]A 1.0 mg/kg dose and a higher dose (3.0 mg/kg) of Risperidone are chosen for study. Beginning on postnatal day 14, subcutaneous injections of Risperidone are performed daily until postnatal day 42. Within each study, three groups of roughly equal numbers of rats receive injections of 1.0 mg/kg of Risperidone, 3.0 mg/kg of Risperidone, or the vehicle used for the Risperidone solution as a control. Within each litter, there are 1-2 pups of the same sex that receive the same treatment. Injections of Risperidone are performed in a room just outside of the housing room. Prior to weaning, the pups are removed from the home cage and placed in a separate cage during injections[2]. |
参考文献: [1]. Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cellapoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. | |
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