Biphenyl-indanone A (BINA) is a potent selective positive allosteric modulator for the group II metabotropic glutamate receptor subtype mGluR2. In animal studies BINA showed anxiolytic and antipsychotic effects, and blocked the effects produced by the hallucinogenic drug DOB. It decreased cocaine self-administration in rats, with no effect on food self-administration. In recombinant systems, BINA selectively potentiated the response of mGluR2 to glutamate with no effect on the glutamate response of other mGluR receptor subtypes tested.
Biphenyl-indanone A is a potent selective positive allosteric modulator for the group II metabotropic glutamate receptor subtype mGluR2.
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Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 43(13), 2615-2626 (2018-10-05)
Opioid abuse is a rapidly growing public health crisis in the USA. Despite extensive research in the past decades, little is known about the etiology of opioid addiction or the neurobiological risk factors that increase vulnerability to opioid use and
British journal of pharmacology, 174(24), 4785-4796 (2017-10-03)
We recently proposed the existence of mGlu We studied the effect of LY566332, an mGlu Cortical synaptosomes possess LY566332-sensitive autoreceptors that are slightly, although significantly, susceptible to LY2389575. In contrast, LY566332-insensitive and LY2389575-sensitive autoreceptors are present in spinal cord terminals.
While many orthosteric ligands have been developed for the mGlu2 receptor, little is known about their target binding kinetics and how these relate to those of the endogenous agonist glutamate. Here, the kinetic rate constants, i.e. kon and koff, of
G protein coupled receptors (GPCRs) play essential roles in intercellular communication. Although reported two decades ago, the assembly of GPCRs into dimer and larger oligomers in their native environment is still a matter of intense debate. Here, using number and
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