Potent, selective positive allosteric modulator for mGlu1 (pEC50 = 7.16 for rat mGlu1a receptors). Increases basal mGluR1-induced cAMP accumulation and potentiates glutamate-induced cAMP accumulation. Selectively enhanced responses to DHPG in vivo (EC50= 95 nM in CA3 neurons).
Store at Room Temperature. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Sheffler DJ & Conn PJ Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology55:419-27 (2008).
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Hemstapat K et al. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol Pharmacol70:616-26 (2006).
Read more (PubMed: 16645124) »
Knoflach F et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A98:13402-7 (2001).
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