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. 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].

12352005

5-HT Receptor; Dopamine Receptor; MMP

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Neurological Disease

O=S(C1=CC=C(F)C=C1)(NC2CCN(CCOC3=CC=CC=C3C4=CN(C)N=C4)CC2)=O.Cl

C23H28ClFN4O3S

495.01

[1]Canale V, et al. Fine-tuning 5-HT7 receptor selectivity, inverse agonism, and metabolic stability of new (aryloxy) ethyl-piperidines toward antidepressant and pro-cognitive properties. Eur J Med Chem. 2026 Jan 15;302 (Pt 3) :118369.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-179724A/

Reference compound1

No Development Reported

5-HT1 Receptor;5-HT2 Receptor;5-HT6 Receptor;5-HT7 Receptor; D2 Receptor; MMP-9