Selective mGlu1 receptor non-competitive antagonist
CAS：232605-26-4
分子式：C19H18O2
分子量：278.35
纯度：98%
存储：Store at -20°C

Background:

Metabotropic glutamate (mGlu) receptors are G proteincoupled receptors (GPCRs) that act predominantly as modulators of synaptic transmission. As such, they play a role in many physiological and pathophysiological processes. BAY36-7620 is a pPotent non-competitive mGlu1 receptor antagonist with.

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].

Clinical trial: Up to now, BAY 36-7620 is still in the preclinical development stage.

Reference:
[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.