Pharmacological characterization of metabotropic glutamate receptors linked to the inhibition of adenylate cyclase activity in rat striatal slices
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Cited by (27)
In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu<inf>2/3</inf> receptor antagonist
2017, NeuropharmacologyCitation Excerpt :With an understanding of rat brain binding affinity for LY3020371 in place, we desired to establish the functional antagonist potency of LY3020371 on agonist-mediated second messenger levels in a representative brain region. The ability of selective mGlu2/3 receptor agonists to inhibit stimulated cAMP production in intact slice preparations (Schoepp et al., 1995, 1998; Iacovelli et al., 2009) and antagonists to block this agonist-mediated response (Schaffhauser et al., 1997; Schoepp et al., 1998) is well established. While synaptosome (presynaptic terminal) preparations (Whittaker et al., 1964; Whittaker, 1993) have been successfully utilized to evaluate the ability of mGlu2/3 receptor agonists to influence evoked transmitter release from cortical (Attwell et al., 1998a,b), striatal (Mela et al., 2006) and spinal cord preparations (Romei et al., 2013), to the best of our knowledge, these elements derived from presynaptic terminals have not been employed in the study of selective mGlu2/3 agonists or antagonists on second messenger production, although a single study utilizing the non-selective mGlu receptor agonist 1S,3R-ACPD (Musgrave et al., 1994) and studies of other presynaptic mechanisms (Steffens et al., 2005; Chen et al., 2013) support technical feasibility.
Sustained behavioral stimulation following selective activation of group I metabotropic glutamate receptors in rat striatum
2000, Pharmacology Biochemistry and Behavior