PZ-1657 hydrochloride
PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder.
For research use only. We do not sell to patients.
- Formula: C23H28ClFN4O3S
- Molecular Weight:495.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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5-HT7 Receptor 5 nM (Ki) |
5-HT1A Receptor 292 nM (Ki) |
5-HT2A Receptor 435 nM (Ki) |
D2 Receptor 1004 nM (Ki) |
5-HT6 Receptor 3282 nM (Ki) |
MMP-9 |
| Species | Dose | Route | Note | AUC0-t | MRT | T1/2 | Cmax | Tmax | F | CL | Vss |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.g. | brain | 14399 min·ng/mL | 117.9 min | 153.9 min | 78.9 ng/mL | 120 min | / | / | / |
| Rat[1] | 10 mg/kg | i.g. | plasma | 55900 min·ng/mL | 56.6 min | 68.9 min | 1056.7 ng/mL | 15 min | 57.2 % | / | / |
| Rat[1] | 2 mg/kg | i.v. | brain | 59513 min·ng/mL | 89.9 min | 137.4 min | 527 ng/mL | / | / | / | / |
| Rat[1] | 2 mg/kg | i.v. | plasma | 19552 min·ng/mL | 55.1 min | / | / | / | 100 % | 84.6 mL/min/kg | 10 L/kg |
Chemical Information
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Molecular Weight 495.01
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Formula C23H28ClFN4O3S
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SMILES
O=S(C1=CC=C(F)C=C1)(NC2CCN(CCOC3=CC=CC=C3C4=CN(C)N=C4)CC2)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PZ-1657 hydrochloride Related Classifications
HY-179724A Related Classifications
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