piclozotan

Piclozotan is an investigational small molecule drug that acts as a selective agonist at the serotonin 1A (5-hydroxytryptamine receptor 1A) receptor. It is a derivative of 1,4-benzoxazepine and exhibits sub-nanomolar affinity for the serotonin 1A receptor with good selectivity over dopamine D2 and α₁-adrenoceptors. Preclinical studies have shown that piclozotan can reduce levodopa-induced dyskinesia and modulate striatal dopamine levels in animal models of Parkinson's disease. Additionally, it has demonstrated neuroprotective effects against ischemic neuronal damage in animal models of stroke. Clinical development reached Phase II trials for both Parkinson's disease (to address motor complications such as dyskinesia) and acute ischemic stroke; however, further development appears to have been discontinued[8][5][2].

Other names

Piclozotan182415-09-4Piclozotan [INN]UNII-FQE44HS7AHUNII-FQE-44HS7AHUNII-FQE 44HS7AHFQE44HS7AHFQE-44HS7AHFQE 44HS7AHpiclozotanum3-chloro-4-(4-(4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl)butyl)-1,4-benzoxazepin-5(4H)-one3-chloro-4-(4-{1',2',3',6'-tetrahydro-[2,4'-bipyridine]-1'-yl}butyl)-4,5-dihydro-1,4-benzoxazepin-5-one