For research use only. Not for therapeutic Use.
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM[1][2]. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM)[3].
In the Purkinje cells of rat cerebellar slices, Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5[3].?
Ro 67-7476 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM). The EC50?value of? full P-ERK1/2 activation for Ro 67-7476 are nearly identical to the EC50 for calcium mobilization potentiation[3].Ro 67-7476 increases basal cAMP production approximately by 8%. It potentiated threshold responses to glutamate in the cAMP accumulation assay, with an EC50?value of 17.7 μM[3].
| Catalog Number | I003033 |
| CAS Number | 298690-60-5 |
| Synonyms | (2S)-2-(4-fluorophenyl)-1-(4-methylphenyl)sulfonylpyrrolidine |
| Molecular Formula | C17H18FNO2S |
| Purity | ≥95% |
| InChI | InChI=1S/C17H18FNO2S/c1-13-4-10-16(11-5-13)22(20,21)19-12-2-3-17(19)14-6-8-15(18)9-7-14/h4-11,17H,2-3,12H2,1H3/t17-/m0/s1 |
| InChIKey | DAEHFYNGSSBGSS-KRWDZBQOSA-N |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)N2CCCC2C3=CC=C(C=C3)F |
| Reference | [1]. F Knoflach, et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7 [2]. Kamondanai Hemstapat, 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 Pharmacol. 2006 Aug;70(2):616-26. [3]. Douglas J Sheffler, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008 Sep;55(4):419-27 |
