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Ziprasidone mesilate

Names

[ CAS No. ]:
199191-69-0

[ Name ]:
Ziprasidone mesilate

[Synonym ]:
5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2h-indol-2-one
anhydrous 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one
Ziprasidone
Ziprasidone mesilate
2H-INDOL-2-ONE,5-[2-[4-(1,2-BENZISOTHIAZOL-3-YL)-1-PIPERAZINYL]ETHYL]-6-CHLORO-1,3-DIHYDRO-,MONOMETHANESULFONATE,TRIHYDRATE
[14C]-Ziprasidone
5-[2-[4-(1,2-benzisothiazol-3yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one mesilate
[3H]-Ziprasidone
Ziprasidone mesylate trihydrate
5-{2-[4-(1,2-Benzothiazol-3-yl)-1-piperazinyl]ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one methanesulfonate hydrate (1:1:3)
2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, methanesulfonate, hydrate (1:1:3)
ZIPRASIDONE MESYLATE

Biological Activity

[Description]:

Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

Rat 5-HT2 Receptor:0.42 nM (Ki)

Rat 5-HT1A Receptor:3.4 nM (Ki)

Rat D2 Receptor:4.8 nM (Ki)


[In Vitro]

Ziprasidone mesylate trihydrate (0-500 nM, 150 seconds) blocks wild-type hERG current[2]. Cell Viability Assay Cell Line: HEK-293 cells[2] Concentration: 0-500 nM Incubation Time: 150 seconds Result: Blocked wild-type hERG current in a voltage- and concentration-dependent manner (IC50 = 120 nm).

[In Vivo]

Ziprasidone mesylate trihydrate (oral gavage; 20 mg/kg; once daily; 7 weeks) results in weight loss, low level physical activity, high resting energy expenditure and greater capacity for thermogenesis when subjected to cold[3]. Animal Model: Eight-week-old female Sprague-Dawley rats weighing 200 to 250 g[3] Dosage: 20 mg/kg Administration: Oral gavage; 20 mg/kg; once daily; 7 weeks Result: Gained significantly less weight (P = 0.031), had a lower level of physical activity (P = 0.016), showed a higher resting energy expenditure (P < 0.001), and displayed a greater capacity for thermogenesis when subjected to cold (P < 0.001).

[References]

[1]. H Rollema, et al. 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry. 2000 Aug 1;48(3):229-37.

[2]. Zhi Su, et al. Block of hERG channel by ziprasidone: biophysical properties and molecular determinants. Biochem Pharmacol. 2006 Jan 12;71(3):278-86.

[3]. Subin Park, et al. The effect of ziprasidone on body weight and energy expenditure in female rats. Metabolism. 2012 Jun;61(6):787-93.

Chemical & Physical Properties

[ Boiling Point ]:
554.8ºC at 760 mmHg

[ Molecular Formula ]:
C22H31ClN4O7S2

[ Molecular Weight ]:
563.087

[ Exact Mass ]:
562.132263

[ PSA ]:
167.15000

[ LogP ]:
4.34180

[ Vapour Pressure ]:
1.13E-29mmHg at 25°C

Related Compounds