Ontology highlight
ABSTRACT:
SUBMITTER: Weston M
PROVIDER: S-EPMC6469940 | biostudies-literature | 2019 Apr
REPOSITORIES: biostudies-literature
Weston Mikail M Kaserer Teresa T Wu Angela A Mouravlev Alexandre A Carpenter Jenna C JC Snowball Albert A Knauss Samuel S von Schimmelmann Melanie M During Matthew J MJ Lignani Gabriele G Schorge Stephanie S Young Deborah D Kullmann Dimitri M DM Lieb Andreas A
Science advances 20190417 4
Designer receptors exclusively activated by designer drugs (DREADDs) derived from muscarinic receptors not only are a powerful tool to test causality in basic neuroscience but also are potentially amenable to clinical translation. A major obstacle, however, is that the widely used agonist clozapine <i>N</i>-oxide undergoes conversion to clozapine, which penetrates the blood-brain barrier but has an unfavorable side effect profile. Perlapine has been reported to activate DREADDs at nanomolar conc ...[more]