BAY36-7620 is a non-competitive, potent and selective metabotropic glutamate mGlu1 receptor (mGluR1) antagonist (IC50 = 160 nM against 0.1 μM (EC50) Glu-stimulated IP) with inverse agonist activity (IC50 = 380 nM with 36-44% basal IP inhibition at 10 μM). BAY36-7620 exhibits neuroprotective (0.01 and 0.03 mg/kg/h, iv. infusion during 4h post acute subdural hematoma induction in rats; triple 0.03-3 mg/kg bolus iv. 0, 2 & 4 h post middle cerebral artery occlusion in rats) and anticonvulsive (MED = 10 mg/kg, iv. immediately after pentylenetetrazole-induced convulsions in mice) efficacy in vivo.
Non-competitive, potent and selective metabotropic glutamate mGlu1 receptor (mGluR1) antagonist with neuroprotective and anticonvulsive efficacy in vivo.
European journal of pharmacology, 428(2), 203-214 (2001-10-25)
This study characterized the neuroprotective and behavioral effects of (3aS,6aS)-6a-naphtalen-2-ylmethyl-5-methyliden-hexahydro-cyclopenta[c]furan-1-on (BAY 36-7620), a novel, selective and systemically active metabotropic glutamate (mGlu)(1) receptor antagonist. In the rat, neuroprotective effects were obtained in the acute subdural hematoma model (efficacy of 40-50% at
American journal of human genetics, 101(3), 451-458 (2017-09-09)
The metabotropic glutamate receptor 1 (mGluR1) is abundantly expressed in the mammalian central nervous system, where it regulates intracellular calcium homeostasis in response to excitatory signaling. Here, we describe heterozygous dominant mutations in GRM1, which encodes mGluR1, that are associated
In this study we evaluated the effects of the novel, potent non-competitive metabotropic glutamate receptor (mGluR) 1 antagonist (3aS,6aS)-6a-naphthalen-2-ylmethyl-5-methyliden-hexahydro-cyclopental[c]furan-1-on (BAY 36-7620) on different types of synaptic plasticity in the hippocampal cornu ammonis (CA) 1-region and on hippocampus-dependent spatial learning. After
Breast cancer remains a major cause of death among women. 15% of these cancers are triple negative breast cancer (TNBC), an aggressive subtype of breast cancer for which no current effective targeted therapy exists. We have previously demonstrated a role
Exosomes are naturally occurring membrane-bound nanovesicles generated constitutively and released by various cell types, and often in higher quantities by tumor cells. Exosomes may facilitate communication between the primary tumor and its local microenvironment, supporting cell invasion and other early
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