(+)-(S)-trujillon, (+)-(S)-4-(2,2-diphenyl-1,3,2-oxazabolidin-5-oxo)propionic acid, a novel glutamatergic analog, modifies the activity of globus pallidus neurons by selective NMDA receptor activation.

Decreased levels of glutamate and changes in several markers of glutamatergic function occur in movement disorders and chronic psychiatric illnesses. Ionotropic glutamate receptors have been implicated in neuronal cell death, and have, therefore, been related to the process of neurodegenerative diseases. Drugs that interact with the glutamatergic system are important tools for the development of better therapies.

In vivo effects of local activation and blockade of 5-HT1B receptors on globus pallidus neuronal spiking.

Several morphological works have shown that the globus pallidus (GP) contains the highest density of 5-HT1B receptors within the telencephalon. However, the role of these receptors in the spiking of GP neurons in vivo is unknown. In the present work, we use single-unit extracellular recordings in the anesthetized rat to analyze changes in the firing rate of GP neurons evoked by local activation and blockade of 5-HT1B receptors.

Stereospecific activity of two glutamate analogs.

Two glutamic acid analogs, (+)-(S)- and (-)-(R)-4-(2,2-diphenyl-1,3,2-oxazaborolidin-5-oxo)propionic acid ((+)-(S)- and (-)-(R)-Trujillon, respectively), were prepared. The stereospecific activity of their pharmacological properties was studied. The median convulsant dose (CD(50)) and median lethal dose (LD(50)) were analyzed in female Swiss Webster mice and their effects in vivo on unitary electrical activity in globus pallidus neurons were elucidated in male Wistar rats.

["De Morbis Artificum Diatriba." 1700-2000. ].

Bernardino Ramazzini was a renowned physician and a prolific writer, born in Capri in 1633. He is considered the father of occupational medicine for having written the first paper on workers' diseases (De morbis artificum diatriba). His Treaty on Workers' diseases included 53 different professions, one particular and specific method of analysis, and a methodological proposal to prevent these diseases.