U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Paliperidone (9-OH-risperidone) is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. Very common adverse effects are: headache, tachycardia, somnolence and insomnia.
Status:
Investigational
Source:
NCT02561000: Phase 2 Interventional Completed Arterial Occlusive Diseases
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

PZ-128 (also known as P1pal7 ) is a cell-penetrating pepducin inhibitor of PAR1 that targets the receptor-G-protein interface on the inside surface of platelets. In preclinical studies, PZ-128 suppresses PAR1 aggregation and arterial thrombosis in guinea pigs and baboons and strongly synergized with oral clopidogrel. PZ-128 shows potent anti-metastatic and anti-angiogenic activity in Breast, Ovarian, and Lung Cancer preclinical studies. In clinical trials, PZ-128 shows a promising antiplatelet activity that provides rapid, specific, dose-dependent, and reversible inhibition of platelet protease-activated receptor-1 through a novel intracellular mechanism.
Status:
Investigational
Source:
NCT03748758: Phase 1 Interventional Completed Healthy Adult Volunteers
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Designated
Source:
FDA ORPHAN DRUG:640618
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)