| Identification | Back Directory | [Name]
Pentiapine | [CAS]
81382-51-6 | [Synonyms]
Pentiapine
5-(4-Methyl-1-piperazinyl)imidazo[2,1-b][1,3,5]benzothiadiazepine
CGS10746,Pentiapine,inhibit,Inhibitor,CGS-10746,Dopamine Receptor
Imidazo[2,1-b][1,3,5]benzothiadiazepine, 5-(4-methyl-1-piperazinyl)- | [Molecular Formula]
C15H17N5S | [MDL Number]
MFCD09838073 | [MOL File]
81382-51-6.mol | [Molecular Weight]
299.39 |
| Chemical Properties | Back Directory | [Melting point ]
141-144 °C(Solv: isopropanol (67-63-0)) | [Boiling point ]
548.2±60.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mg/mL (334.01 mM) | [form ]
Solid | [pka]
7.21±0.42(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites[1][2]. | [Definition]
ChEBI: Pentiapine is an aryl sulfide. | [in vivo]
Pentiapine is a novel dopamine release inhibitor.The results show that Pentiapine dose-dependently reduces motor activity of mice. Moreover, Pentiapine dose-dependently reduces morphine-induced hyperactivity. Newman-Keuls post-hoc comparisons indicate that the group receiving morphine plus saline presents more activity than the groups receiving morphine plus 2 (P<0.05), 4, 8, 16, 24 and 32 (P<0.01) mg/kg of Pentiapine. Moreover, the groups receiving morphine plus 0.5, 1 and 2 mg/kg of Pentiapine present more activity than the groups receiving morphine plus 4, 8, 16, 24 and 32 mg/kg of Pentiapine (P<0.01)[1]. 30 mg/kg dose of Pentiapine completely blocks the methylenedioxymethamphetamine (MDMA) conditioned place preference (CPP) and also blocks the establishment of a cocaine CPP[2]. | [storage]
Store at -20°C | [References]
[1] Manzanedo C, et al. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32. DOI:10.1016/s0166-4328(01)00237-6
[2] Bilsky EJ, et al. CGS 10746B, a novel dopamine release inhibitor, blocks the establishment of cocaine and MDMA conditioned place preferences. Pharmacol Biochem Behav. 1998 Jan;59(1):215-20. DOI:10.1016/s0091-3057(97)00424-3 |
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