Publications by authors named "Danette M Pascarella"
Article Synopsis
- Activation of M1 muscarinic receptors involves both orthosteric and allosteric binding sites, and researchers used site-directed mutagenesis to identify key residues affecting their function.
- Specific amino acids were found critical for the agonist activity of compounds like AC-42 and TBPB, while N-desmethylclozapine engaged a different binding site without relying on those same residues.
- The study indicates that various structurally different allosteric agonists can interact with distinct regions of the M1 receptor, suggesting multiple pathways for receptor activation.
Multiple studies indicate that N-methyl-D-aspartate (NMDA) receptor hypofunction underlies some of the deficits associated with schizophrenia. One approach for improving NMDA receptor function is to enhance occupancy of the glycine modulatory site on the NMDA receptor by increasing the availability of the endogenous coagonists D-serine. Here, we characterized a novel D-amino acid oxidase (DAAO) inhibitor, compound 8 [4H-thieno [3,2-b]pyrrole-5-carboxylic acid] and compared it with D-serine.
View Article and Find Full Text PDFMice deficient in the neurotensin (NT)-1 receptor (NTR1) were developed to characterize the NT receptor subtypes that mediate various in vivo responses to NT. F2 generation (C57BL6/Sv129J) NTR1 knockout (-/-) mice were viable, and showed normal growth and overt behavior. The -/- mice lacked detectable NTR1 radioligand binding in brain, whereas NTR2 receptor binding density appeared normal compared with wild-type (+/+) mice.
View Article and Find Full Text PDF