Ziprasidone hydrochloride monohydrate CAS: 138982-67-9
MF: C21H21ClN4OS•HCl•H2O
MW: 467.4
An SR-2A and D2DR inhibitor.

Ziprasidone hydrochloride monohydrate (CAS 138982-67-9)

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Application: An SR-2A and D2DR inhibitor
CAS Number: 138982-67-9
Purity: ≥98%
Molecular Weight: 467.4
Molecular Formula: C21H21ClN4OS•HCl•H2O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ziprasidone hydrochloride monohydrate is an atypical antipsychotic that displays combined SR-2A and D2DR inhibition. Ziprasidone displays high affinity at SR-2A receptors with a SR-2A/D2DR affinity ratio greater than any other clinically available atypical antipsychotics (pKi values are 9.38, 8.88, 8.69, 8.47, 8.32, 8.14, 7.98, 7.49, 7.33 and 6.28 for SR-2A, 5-HT2C, 5-HT1D, 5-HT1A, D2DR, D3, α1, D4, H1 and D1 receptors respectively).


References

Seeger et al (1995) Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J.Pharmacol.Exp.Ther. 275 101. Schmidt et al (2001) Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile. Eur.J.Pharmacol. 425 197. Fell et al (2005) Investigation into the effects of the novel antipsychotic ziprasidone on weight gain and reproductive function in female rats. Behav.Brain Res. 160 338.

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (>10 mg/ml), DMF (~0.16 mg/ml), and 1: 2 solution of DMSO: PBS (pH 7.2) (~0.33 mg/ml). Insoluble in water.
Storage :
Store at room temperature
Melting Point :
>300° C
Boiling Point :
554.8° C at 760 mmHg (Predicted)
Refractive Index :
n20D 1.75 (Predicted)
IC50 :
SR-2A: IC50 = 0.42 nM (human); D2DR: IC50 = 5 nM (human); Adrenergic receptor α-1: IC50 = 11 nM (human); HERG: IC50 = 120.23 nM (human); Histamine H1 receptor: IC50 = 150 nM (rat)
Ki Data :
SR-2A: Ki= 0.08 nM (human); Dopamine D2 receptor and Serotonin 2a receptor: Ki= 0.42 nM (rat); α-1a adrenergic receptor: Ki= 0.5 nM (rat); 5-HT1A agonist: Ki= 3.4 nM; D2 receptor: Ki= 4.8 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
60853
Merck Index :
14: 10171
MDL Number :
MFCD00921885
SMILES :
C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.O.Cl

Download SDS (MSDS)

Certificate of Analysis

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