PURPOSE Iloperidone, second generation antipsychotic drug, reported in clinical trial to produce orthostatic hypotension as side effect. It was claimed to be antagonistic at alpha adrenergic receptor in central nervous system. We evaluated effect of Iloperidone on peripheral alpha 1 adrenoreceptor by in silico and in vitro methods while in vivo hypotensive, antihypertensive and ocular hypotensive activity was evaluated in animals. METHODS Pharmacological activity prediction of Iloperidone was done using PASSOnline and SwissTargetPrediction softwares and molecular docking with Alpha 1A adrenoreceptor using AutoDock Vina. Hypotensive activity in normotensive and antihypertensive activity against DOCA-salt induced hypertension in rats were evaluated at doses 0.03 mg/Kg and 0.1 mg/Kg, i.p of Iloperidone. Blood pressure was measured by invasive blood pressure measurement technique using PowerLab 4/30 and intraocular pressure was measured using digital tonometer. RESULTS Iloperidone (0.1 mg/Kg) showed significant decrease in blood pressure (38.96 ± 1.1%) in normotensive rats, while in DOCA salt induced hypertensive rats, systolic blood pressure was found to be decreased by 29.04 ± 1.45% and 31.43 ± 1.21% in 0.03 mg/Kg and 0.1 mg/Kg treated rats respectively. Iloperidone prevented rise in systolic BP with adrenaline. Intraocular pressure was found to be decreased by 36.66 ± 3.15% in rabbits after 1 h of instillation of 0.1% Iloperidone. CONCLUSION Iloperidone exerted hypotensive and/or anti-hypertensive activity in rats and ocular hypotensive activity in rabbits.

中文翻译：

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利必利酮的再利用：动物的降压和眼压降压活动。

目的第二代抗精神病药伊潘立酮在临床试验中报道会产生立位性低血压作为副作用。据称它对中枢神经系统的α肾上腺素能受体具有拮抗作用。我们通过计算机和体外方法评估了伊潘立酮对外周血α1肾上腺素受体的影响，同时在动物体内评估了体内降压，抗高血压和眼部降压活性。方法使用PASSOnline和SwissTargetPrediction软件进行伊潘立酮的药理活性预测，并使用AutoDock Vina与Alpha 1A肾上腺素受体进行分子对接。在腹腔注射伊潘立酮的剂量为0.03 mg / Kg和0.1 mg / Kg时，评估了对DOCA-盐诱导的高血压大鼠的降压活性和降压活性。通过使用PowerLab 4/30的有创血压测量技术测量血压，并使用数字眼压计测量眼内压。结果依普利酮（0.1 mg / Kg）在血压正常的大鼠中血压显着下降（38.96±1.1％），而在DOCA盐诱导的高血压大鼠中，收缩压被发现下降29.04±1.45％和31.43±1.21％分别以0.03 mg / Kg和0.1 mg / Kg的剂量处理大鼠。伊潘立酮预防肾上腺素使收缩压升高。在滴注0.1％伊立立酮1小时后，发现兔眼内压降低了36.66±3.15％。结论伊潘立酮在大鼠中具有降压和/或抗高血压活性，在兔中具有眼降压活性。