https://sciencematters.io/articles/201712000006
Lumateperone is a compound in clinical development as a treatment for schizophrenia, bipolar depression, agitation associated with dementia and other neuropsychiatric and neurodegenerative diseases. This novel compound exhibits high affinity in vitro binding to dopamine D2 receptors and occupies striatal dopamine D2 receptors in human brain at therapeutic doses. At dopamine D2 receptors lumateperone displays dual properties, acting both as a functional post-synaptic antagonist and pre-synaptic partial agonist. To further characterize these unique receptor interactions, we compared the activity of lumateperone relative to three known D2 partial agonists of differing intrinsic efficacy, aripiprazole, brexpiprazole, and bifeprunox, in cell-based functional assays that permit characterization of compounds of differing intrinsic efficacy (e.g. full agonism to neutral antagonism). Lumateperone had no demonstrable agonist activity in CHO cells expressing recombinant human D2L (or D2S) receptors, in assays where other known partial agonists displayed different degrees of agonist activity.
2 Likes
Is it good for negative symptoms …!!! @jamesbond …!!!
I think so!
1 Like