Z-Cyclopentyl-AP4A Group III mGluR (mGluR-4,6) agonist

Z-Cyclopentyl-AP4 (CAS 103439-17-4)

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Application: A Group III mGluR (mGluR-4,6) agonist
CAS Number: 103439-17-4
Molecular Weight: 209.14
Molecular Formula: C6H12NO5P
* Refer to Certificate of Analysis for lot specific data (including water content).
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Z-Cyclopentyl-AP4 is a Group III mGluR agonist that displays higher potency at mGluR-4 than mGluR-8 (EC50 values are 49 and 124 µM respectively) with no activity at mGluR-7. Z-Cyclopentyl-AP4 also selectively inhibits synaptic activity in the lateral perforant pathway (IC50 values are 130 and 1859 μM in the lateral and medial perforant pathways respectively). Conformationally restrained analog of L-AP4 (sc-200432).


References

Crooks et al (1986) Cyclic analogues of 2-amino-4-phosphonobutanoic acid (APB) and their inhibition of hippocampal excitatory transmission and displacement of [3H]APB binding. J.Med.Chem. 29 1988. Ayala et al (2008) Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated. Neuropharmacology 54 804. Jones et al (2008) Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract-piriform cortex synpase. Neuropharmacology 55 440.

Physical State :
Solid
Solubility :
Soluble in 1.1eq. NaOH (50 mM), and water (partly).
Storage :
Store at 4° C
IC50 :
mGluR-4 : EC5050 = 49 µM; mGluR-8 : EC5050 = 124 µM; Synaptic activity: IC50 = 130 µM (lateral perforant pathway); Synaptic activity: IC50 = 1859 µM (medial perforant pathway)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
MDL Number :
MFCD12828753

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Certificate of Analysis

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