N-Acetylaspartylglutamate is not demonstrated to be a selective mGlu3 receptor agonist

The neuroactive peptide N-acetylaspartylglutamate is not an agonist at the metabotropic glutamate receptor subtype 3 of metabotropic glutamate receptor.

The peptide N-acetylaspartylglutamate (NAAG) is present in high concentrations in the mammalian central nervous system. Various mechanisms have been proposed for its action, including selective activation of the metabotropic glutamate receptor (mGluR) subtype 3, its action at the N-methyl-D-aspartate receptor, or the production of glutamate by its hydrolysis catalyzed by an extracellular protea...

“Not Everything That Is Faced Can Be Changed, but Nothing Can Be Changed Until It Is Faced”: A Response to Recent Commentaries

Vesicular uptake of N-acetylaspartylglutamate is catalysed by sialin (SLC17A5).

NAAG (N-acetylaspartylglutamate) is an abundant neuropeptide in the vertebrate nervous system. It is released from synaptic terminals in a calcium-dependent manner and has been shown to act as an agonist at the type II metabotropic glutamate receptor mGluR3. It has been proposed that NAAG may also be released from axons. So far, however, it has remained unclear how NAAG is transported into syna...

Ischemic Neuroprotection With Selective -Opioid Receptor Agonist Is Gender Specific

Background and Purpose—We demonstrated previously that treatment with selective -opioid receptor (KOR) agonist BRL 52537 hydrochloride [( )-1-(3,4-dichlorophenyl) acetyl-2-(1-pyrrolidinyl) methylpiperidine] (1) has a long therapeutic window for providing ischemic neuroprotection, and (2) attenuates ischemia-evoked NO production in vivo in rats. Neuronally derived NO has been shown to be deleter...

The pyrazolone originally reported to be a formyl peptide receptor (FPR) 2/ALX-selective agonist is instead an FPR1 and FPR2/ALX dual agonist.

A pyrazolone compound acting as a formyl peptide receptor (FPR) 2/ALX-selective agonist has been reported, but its pharmacological activities on human FPRs (hFPRs) and mouse FPRs (mFprs) have not been well demonstrated. In this study, we found that this compound, designated as compound A, induced concentration-dependent calcium flux not only in Chinese hamster ovary (CHO) cells expressing hFPR2...