60 products were found matching "K04603"!

(S)-3,5-DHPG, known more commonly as DHPG, is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 µM, respectively) but not ionotropic glutamate receptors. The (S)-enantiomer is about ten times more potent than the (R)-enantiomer. (S)-3,5-DHPG is...

An antagonist of mGluR1 (IC50 = 140 nM), reduces the growth of PC-9 cells and PC-9-AMG cells in MGS co-culture but not in monoculture, reduces MGS co-culture-induced increases in EGFR levels in PC-9-AMG cells, reduces tumor growth in a PC-9-AMG mouse model of brain metastasis at 50 mg/kg per day, inhibits seizures...

Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 µM). It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 µM. Ro 67-7476 increases the...

CPCCOEt is a low affinity, selective, non-competitive antagonist of the metabotropic glutamate receptor subtype mGluR1b. It has been shown to inhibit glutamate-induced increases in intracellular calcium at human mGluR1b with an IC50 value of 6.5 µM while having no agonist or antagonist activity at mGluR2, -4a, -5a,...

(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...

Anti-mGluR1a antibodies are affinity purified from monospecific antiserum by immunoaffinity purification. Immunolabeling blocked by preadsorption of antibody with the peptide used to generate the antibody. This antibody is directed against rat mGluR1a. Reactivity is expected from mouse. Cross reactivity from other...

A-841720 is a noncompetitive antagonist of the group 1 metabotropic glutamate receptor mGluR1 with an IC50 value of 10.7 nM for inhibition of L-glutamate-induced calcium release in 1321 N1 cells. It is selective for mGluR1 over mGluR5 (IC50 = 343 nM) as well as mGluR2, mGluR4, and mGluR7, where it does not inhibit...

ACPT-II is a general competitive antagonist of metabotropic glutamate (mGlu) receptors. The KB values for mGlu1a, mGlu2, and mGlu4a receptors are 115, 88, and 77 µM, respectively. It binds to the large extracellular domain called a Venus flytrap module, where agonists bind. ACPT-II is a stereoisomer of the group III...

YM-298198 is a non-competitive antagonist of the metabotropic glutamate receptor type I (mGluR1, Ki = 19 nM). It is selective for mGluR1 over mGluR2-7 (IC50s = 0.016 and >10 µM, respectively). YM-298198 binds to rat cerebellum membranes (Ki = 20 nM). In vivo, YM-298198 (10 and 30 mg/kg, p.o.) increases nociceptive...

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. May...

(±)-trans-ACPD is an agonist of metabotropic glutamate receptors (mGluRs, EC50s = 15, 2, 40, 23, and 82 µM for mGluR1, -2, -3, -5, and -6, respectively, in CHO cells expressing recombinant receptors). It also activates mGluR4 in baby hamster kidney cells with an EC50 value of approximately 800 µM. (±)-trans-ACPD...