Uses
Bay 36-7620, is an inhibitor of metabotropic glutamate receptor 1 (mGlu1 receptor), and thus suppresses tumor growth and angiogenesis in experimental non-small cell lung cancer (NSCLC).
Biological Activity
Selective mGlu 1 receptor non-competitive antagonist (IC 50 = 0.16 μ M) with inverse agonist activity. Impairs classical conditioning and associated synaptic plasticity in hippocampal neurons. Exhibits neuroprotective and anticonvulsive effects in vivo following systemic administration.
in vitro
bay36-7620 is a potent and selective antagonist at mglu1receptors and inhibits >60% of mglu1a receptor constitutive activity (ic50 = 0.38 μm). bay36-7620 is thus the first described mglu1 receptor inverse agonist. moreover, bay36-7620 did not displace the [3h]quisqualate binding from the glu-binding pocket, indicating that bay36-7620 is a noncompetitive mglu1 antagonist [2].
in vivo
bay 36-7620 protected against pentylenetetrazole-induced convulsions in the mouse. as assessed in rats, bay 36-7620 was devoid of the typical side effects of the ionotropic glutamate (iglu) receptor antagonists phencyclidine and mk-801. therefore, bay 36-7620 did not disrupt sensorimotor gating, induce phencyclidine-like discriminative effects or stereotypical behavior, or facilitate intracranial self-stimulated behavior [3].
IC 50
mGluR 1: 0.16 μM (IC50); mGluR1a: 0.38 μM (IC50); mGluR2: 0.14 μM (IC50); mGluR 5: 0.24 μM (IC50)
References
[1] carroll fy, stolle a, beart pm, voerste a, brabet i, mauler f, joly c, antonicek h, bockaert j, müller t, pin jp, prézeau l. bay36-7620: a potent non-competitive mglu1 receptor antagonist with inverse agonist activity. mol pharmacol. 2001 may;59(5):965-73.
[2] de vry j, horváth e, schreiber r. neuroprotective and behavioral effects of the selective metabotropic glutamate mglu(1) receptor antagonist bay 36-7620. eur j pharmacol. 2001 oct 5;428(2):203-14.
