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The HIV-1 coat protein gp120 and some of its fragments potently activate native cerebral NMDA receptors mediating neuropeptide release by Anita Gemignani; Paolo Paudice; Anna Pittaluga; Maurizio Raiteri is a Neuroscience article available to read on EtoBox.

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## Abstract The objective of this study was to investigate the effects of the HIV‐1 envelope protein gp120 and its peptide fragments on the function of N‐methyl‐ d‐aspartate (NMDA) receptors mediating release of cholecystokinin (CCK) and somatostatin (SRIF). These are nonconventional NMDA receptors recently found to be activated by glycine or d‐serine ‘only’. The release of cholecystokinin‐like immunoreactivity (CCK‐LI) and of somatostatin‐like immunoreactivity (SRIF‐LI) elicited by 12 mm K^+^ from superfused rat neocortex synaptosomes was potently increased by gp120, its cyclic V3 loop and the linear V3 sequence BRU‐C‐34‐A, but not by RP‐135 (a central portion of BRU‐C‐34‐A). The EC~50~ values of gp120 were 0.02 nm (CCK‐LI release) and 0.01 nm (SRIF‐LI release). The releasing effect of gp120 was prevented by blocking the glycine site or the ion channel of NMDA receptors, but not the glutamate recognition site; in addition, the gp120 effect was strongly inhibited by nanomolar concentrations of Zn^2+^ ions and by low micromolar concentrations of ifenprodil. It is concluded that gp120 acts as a very potent agonist at the glycine site of NMDA receptors sited on CCK‐ and SRIF‐releasing

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Author

Anita Gemignani; Paolo Paudice; Anna Pittaluga; Maurizio Raiteri

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0953-816X)

Published

2000

Language

EN

Field

Neuroscience (Life Sciences)