生物活性 | |||
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描述 | Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic. Haloperidol (1 mg) intra-arterially attenuated the dopamine-induced pancreatic secretion. Haloperidol (3 mg) completely inhibits the action of 10 μg of dopamine in the pancreas of the dogs[1]. Large doses of haloperidol can safely be given intravenously and intramuscularly for rapid neuroleptisation; the bioavailability of this agent administered orally ranges from 60 to 65%[3]. The CNS delivery of major fraction of haloperidol via direct transnasal to brain pathway that can be a promising alternative to oral and parenteral routes in chronic and acute situations. Haloperidol concentration of 275.6 ng/g brain 8h post intranasal instillation, higher than therapeutic concentration range of haloperidol (0.8 to 5.15 ng/ml), suggests possible sustained delivery of the drug through nasal route[4]. Moreover, 0.5 mg haloperidol (i.v.) increased latent inhibition in one of two visual tasks. In the task where 0.5 mg haloperidol had enhanced latent inhibition, 1.0 mg had the same effect. In the task where 0.5 mg haloperidol had been ineffective, 1.0 mg haloperidol enhanced latent inhibition in high schizotypal subjects only. Thus, a dose dependence of haloperidol's effects on latent inhibition that parallels results from animal work[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.66mL 0.53mL 0.27mL |
13.30mL 2.66mL 1.33mL |
26.61mL 5.32mL 2.66mL |
参考文献 |
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