Shionogi & Co. Ltd. has synthesized spiroheterocycle derivatives acting as 5-HT2A and 5-HT2C receptor antagonists and/or inverse agonists reported to be useful for the treatment of neurodegeneration.
Chronic inflammatory and neuropathic pain are among the most common chronic conditions, but their treatment options present significant limitations both in efficacy and safety. Researchers from Purdue University presented data on their work aimed to develop adenyl cyclase type 1 (AC1, ADCY1) inhibitors as a new treatment for chronic pain.
As expected, the serotonin-dopamine modulator Rexulti (brexpiprazole) from Otsuka Pharmaceutical Co. Ltd. and H. Lundbeck A/S for agitation in Alzheimer’s disease (AD) dementia, found favor April 14 at the joint meeting of the U.S. FDA’s Psychopharmacologic Drugs Advisory Committee (adcom) and the Peripheral and Central Nervous System Drugs Advisory Committee.
Merck Sharp & Dohme Corp. have identified nicotinic α7 receptor positive allosteric modulators reported to be useful for the treatment of Alzheimer’s and Parkinson’s diseases, and schizophrenia.
Researchers from High Point University recently reported the discovery and preclinical evaluation of a novel class of highly selective dopamine D4 receptor-selective ligands as potential therapeutic candidates for substance use disorders.
Recent Vanderbilt University patents describe metabotropic glutamate mGlu5 receptor negative allosteric modulators reported to be useful for the treatment of amyotrophic lateral sclerosis, Angelman syndrome, anxiety disorder, autism spectrum disorders, substance abuse and dependence, Alzheimer’s disease, diabetes and obesity, among others.
Acid sphingomyelinase (ASM) is a sphingolipid metabolizing enzyme that catalyzes the hydrolysis of sphingomyelin to ceramide. Previous studies revealed high activity of ASM in the blood and brain of old vs. young individuals or mice, and they implicated this enzyme in neurodegenerative disease pathology.
The analysis of thousands of proteins in the brain has revealed the association of astrocytes with obsessive-compulsive disorder (OCD). A proteomic study by researchers from the University of California Los Angeles (UCLA) has identified them in different cellular compartments of astrocytes and neurons. One such protein, the postsynaptic protein SAPAP3, appeared to regulate the organization of the actin cytoskeleton. Its deficit in astrocytes could cause OCD.
Briefing documents suggest smooth sailing for Rexulti (brexpiprazole) at the meeting to deliberate an application to expand the label of the compound from Otsuka Pharmaceutical Co. Ltd. and Lundbeck A/S into agitation related to Alzheimer’s disease (AD) dementia. A joint sit-down on April 14 of the U.S. FDA’s Psychopharmacologic Drugs Advisory Committee (adcom) and the Peripheral and Central Nervous System Drugs Advisory Committee will take up the matter of an add-on indication for Rexulti, a serotonin-dopamine activity modulator for schizophrenia and for the adjunctive treatment of major depressive disorder.