pz1

Pz-1 is an inhibitor of VEGFR2 and RET (rearranged during transfection) tyrosine kinase that blocks the blood supply required for RET-stimulated growth.

PZ15527 is a PROTAC that targets Bcl-xl.

PPZ1 is a novel DAG-activated TRPC3/TRPC6/TRPC7 channels activator.

Carpipramine (free base) is an atypical antipsychotic compound utilized in France and Japan to treat schizophrenia and anxiety. In addition to its neuroinhibitory and anxiolytic effects, it also possesses hypnotic properties. Structurally, carpipramine resembles tricyclic compounds like imipramine and is related to butyrophenones such as haloperidol.

PZ-1922 free base is a brain-penetrant 5-HT6R/5-HT3R antagonist with Ki values of 17 nM and 0.45 nM, respectively. It reversibly inhibits MAO-B (pIC50: 8.93). In rat novel object recognition (NOR) tests, PZ-1922 free base counteracts Scopolamine (SCOP)-induced memory deficits and prevents Aβ-induced memory decline in T-maze tests.

PZ-1657 (Compound 57) is an orally active inverse agonist of the 5-HT7 receptor (5-HT7 receptor), with high selectivity, ability to penetrate the blood-brain barrier, and metabolic stability, demonstrating a Ki value of 5 nM. It effectively inhibits Gs pathway-mediated basal cyclic adenosine monophosphate (cAMP) production, with an EC50 value of 2.93 nM. Additionally, PZ-1657 inhibits CYP3A4P450 (IC50 = 12.2 μM) and affects the hERG channel. This compound also reduces MMP-9 activity mediated by the 5-HT7 receptor and reverses cognitive dysfunction induced by Phencyclidine. PZ-1657 exhibits antidepressant properties.

PZ-1657 hydrochloride (Compound 57) is a potent, selective, and orally active 5-HT7 receptor inverse agonist, with a Ki value of 5 nM. It inhibits constitutive cAMP production mediated by the Gs signaling pathway, with an EC50 value of 2.93 nM. PZ-1657 hydrochloride significantly reduces 5-HT7 receptor-mediated MMP-9 activity in the mouse hippocampus, showing effects comparable to SB-269970. It reverses cognitive deficits induced by phencyclidine in a rat novel object recognition test without affecting spontaneous activity. PZ-1657 hydrochloride is useful for researching affective disorders such as depression and bipolar disorder.

PZ-1129 is a selective ligand for the 5-HT7 receptor (5-HT7 receptor) with a Ki value of 7 nM. It exhibits Ki values of 159 nM for the 5-HT1A receptor and 24 nM for the D2 receptor. PZ-1129 inhibits constitutive cyclic adenosine monophosphate (cAMP) production mediated by the Gs signaling pathway, with an EC50 of 13.7 nM. This compound is applicable for research into affective disorders such as depression and bipolar disorder.

PZ-11 is a thiazolidinedione (thiazolidinedione) derivative with antitumor activity. It induces apoptosis (apoptosis) in cancer cells by downregulating anti-apoptotic genes AIFM1, BAG3, and BIRC3, while regulating pro-apoptotic genes BAD, HRK, CASP10, and CASP10. PZ-11 is applicable for breast cancer research.

PZ-128, a PAR1 antagonist, is used potentially for the treatment of thrombosis.

SRI-29132 is potent; highly permeant of the blood-brain barrier; and selective for LRRK2 kinase activity, therefore effective in attenuating pro-inflammatory responses in macrophages and in rescuing neurite retraction phenotypes in neurons.

PZ-1922 (Compound 16), able to cross the blood-brain barrier, is a dual antagonist for 5-HT6R and 5-HT3R with K i values of 17 nM and 0.45 nM, respectively. It also reversibly inhibits MAO-B with a pIC50 of 8.93. Moreover, PZ-1922 mitigates scopolamine (SCOP)-induced memory deficits in rats as observed in the novel object recognition (NOR) test and hinders Aβ-induced memory impairment in the T-maze test [1].

PZ-1190, a multitarget ligand for serotonin and dopamine receptors, exhibits potential antipsychotic activity in rodents [1].