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 shows SI of 58 and 200 times for 5-HT1A receptor and D2 receptor. 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[1].
Product Specifications
UNSPSC
12352005
Target
5-HT Receptor; Dopamine Receptor; MMP
Related Pathways
GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling
Field of Research
Neurological Disease
Smiles
O=S(C1=CC=C(F)C=C1)(NC2CCN(CCOC3=CC=CC=C3C4=CN(C)N=C4)CC2)=O.Cl
Molecular Formula
C23H28ClFN4O3S
Molecular Weight
495.01
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-HT1 Receptor;5-HT2 Receptor;5-HT6 Receptor;5-HT7 Receptor; D2 Receptor; MMP-9
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