Catalog No.S1483 Synonyms: HP873
Molecular Weight(MW): 426.48
Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
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|Description||Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.|
Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors.  Iloperidone displays higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 nM and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM).  Iloperidone significantly increases dopa accumulation, an index of dopamine turnover in response to D2 receptor blockade, at doses from 0.3 mg/kg to 10 mg/kg i.p. in the striatum and from 1 mg/kg to 10 mg/kg in the nucleus accumbens. 
|In vivo||Iloperidone exerts behavioral effects in pharmacological rats models of disrupted sensorimotor gating consistent with "atypical" antipsychotics, mediated by antagonism of dopaminergic and noradrenergic receptors. Iloperidone (1 and 3 mg/kg) prevents the PPI-disruptive effects of treatment with 1 mg/kg PCP. Iloperidone (0.3 mg/kg) prevents cirazoline-induced PPI deficits, independent of its effects on startle magnitude.  Iloperidone (10 mg/kg) and Melperone (10 mg/kg) produce an equivalent or a smaller increase in DA release in the nucleus accumbens (NAC) of rats, respectively, compared to the mPFC, whereas none of them increase acetylcholine (ACh) release in the NAC. |
-  Kalkman HO, et al. Neuropsychopharmacology, 2001, 25(6), 904-914.
-  Kongsamut S, et al. Eur J Pharmacol, 1996, 317(2-3), 417-423.
-  Szczepanik AM, et al. J Pharmacol Exp Ther, 1996, 278(2), 913-920.
|In vitro||DMSO||27 mg/mL (63.3 mM)|
|Ethanol||4 mg/mL (9.37 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+dd H2O
For best results, use promptly after mixing.
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