83 products were found matching "K04604"!

VU29 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 5 (mGluR5, Ki = 250 nM). It potentiates glutamate-induced calcium flux in primary rat cortical astrocytes (EC50 = 10. nM). VU29 (30 mg/kg) prevents ethanol-induced memory impairments in the novel object recognition test in rats. It also...

Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the...

Dipraglurant is a negative allosteric modulator (NAM) of metabotropic glutamate receptor 5 (mGluR5, Ki = 21 nM). It inhibits glutamate-induced calcium mobilization, inositol monophosphate (IP1) accumulation, and ERK1/2 phosphorylation in HEK293A cells expressing rat mGluR5a (pKBs = 5. 6. and 6. respectively)....

Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the...

Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390...

(R,S)-CHPG is a potent and selective agonist at metabotropic glutamate receptor 5 (mGluR5). In CHO cells, it had an EC50 of 750 µM for calcium mobilization in mGluR5a-expressing cells but was inactive in mGluR1a-expressing cells. In transfected HEK293 cells, (R,S)-CHPG bound mGluR1a and mGluR5a (Kis = 0.9 and 3.9...

CDPPB is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 5 (mGluR5). It potentiates glutamate-induced increases in intracellular calcium in CHO cells expressing mGluR5 (EC50s = 10 and 20 nM for the human and rat receptor, respectively). CDPPB (30 mg/kg, s.c.) inhibits amphetamine-induced...

Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced...

Protein function: G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling activates a phosphatidylinositol-calcium second messenger system and...

Metabotropic glutamate receptors (mGluR1-8) are G protein-coupled receptors that function to modulate brain excitatory signaling via presynaptic, postsynaptic, and glial mechanisms. DL-AP3 is a competitive mGluR1 antagonist that demonstrates a Ki value of 298 µM and an IC50 value of 1mM for rat mGluR1alpha when...

(S)-MCPG is an antagonist of metabotropic glutamate receptors (mGluRs) and the active component of (±)-MCPG, which is selective for Group I and Group II mGluRs. (S)-MCPG inhibits motoneuron depolarization induced by 1-amino-1,3-dicarboxycyclopentane (ACPD) in neonatal rat spinal cord in vitro and ACPD-induced...