Leonard T. Meltzer

TL;DR: In this series, DA agonist activity was found to be highly dependent on the size of the N-alkyl substituent, the saturation level of the six-membered ring, and the mode of attachment of the 2-aminothiazole ring.

TL;DR: Results suggest that selective NMDA receptor antagonism may be interesting for managing LID in Parkinson's disease patients and co-administration of CI-1041 with L-dopa might prevent the induction of dyskinesias.

TL;DR: The hydroxyl propyne and butyne were among the most potent NR1A/2B antagonists from this study and potentiated the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease, but 48 was not active at 30 mg/kg po.

TL;DR: Assessment of the effects of glutamate, as well as specific agonists and antagonists for ionotropic, N-methyl-D-aspartate (NMDA), (R,S)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) and kainate, and metabotropic subtypes of the glutamate receptor, on the neuronal firing activity of midbrain, substantia nigra zona compacta and vent

TL;DR: A heterocyclic piperazine, 7-[3-[4-(2-pyridinyl)-1-piperazinyl]propoxy]-4H-1-benzopyran-4-one (31, PD 119819) has been identified as an extremely selective DA autoreceptor agonist in tests that include [3H]haloperidol binding, inhibition of spontaneous locomotor activity, and inhibition of brain DA synthesis.