LY 354740A highly selective and potent agonist of group II mGluR

LY 354740 (CAS 176199-48-7)

LY 354740 | CAS 176199-48-7 is rated 5.0 out of 5 by 1.
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Synonym: Eglumetad; Eglumegad
Application: A highly selective and potent agonist of group II mGluR
CAS Number: 176199-48-7
Purity: ≥98%
Molecular Weight: 185.18
Molecular Formula: C8H11NO4
* Refer to Certificate of Analysis for lot specific data (including water content).
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LY 354740 is a highly selective and potent mGluR-2/3 (group II mGlu receptor) agonist. LY 354740 has been shown to be a conformationally constrained analog of glutamate with the ability to decrease forskolin-stimulated cAMP formation by more than 90%. Recent studies have found that activation of presynaptic metabotropic mGluR-2/3 induces long lasting inhibition of P/Q-type Ca2+ channels and the cAMP/protein kinase A pathway.


References

1. Schaffhauser, H., et al. 1997. Eur. J. Pharmacol. 334h: 289-297. PMID: 9369360
2. Schoepp, D.D., et al. 1997. Neuropharmacology. 36: 1-11. PMID: 9144636
2. Helton, D.R., et al. 1998. J. Pharmacol. Exp. Ther. 284: 651-660. PMID: 9454811
3. Klodzinska, A., et al. 1999. Neuropharmacology. 38: 1831-1839. PMID: 10608278

Physical State :
Solid
Solubility :
Soluble in 1 eq. NaOH (100 mM).
Storage :
Store at 4° C
Boiling Point :
344.4-408.4° C at 760 mmHg (Predicted)
Density :
1.6 g/cm3 (Predicted)
Refractive Index :
n20D 1.62 (Predicted)
Optical Activity :
α20/D +26°, c = 1 in 1N HCl
IC50 :
mGlu2 receptor: EC5050 = 5.1 nM; mGlu3 receptor: EC5050 = 24.3 nM; Glutamate receptor ionotropic, AMPA: IC50 >100 µM (rat); Glutamate NMDA receptor: IC50 >100 µM (rat); Glutamate receptor ionotropic, kainate: IC50 >100 µM (rat)
Ki Data :
mGluR-2: Ki= 11 nM (human); Metabotropic glutamate receptor 2: Ki= 23.4 nM (rat); mGluR-3: Ki= 38 nM (human); Metabotropic glutamate receptor 3: Ki= 53.5 nM (rat); mGluR-6: Ki= 3 µM (human)
pK Values :
pKa: 2.06 (Predicted), pKb: 9.75 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
DT7324500
PubChem CID :
213056
MDL Number :
MFCD04113018
SMILES :
C1C[C@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(C(=O)O)N

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LY 354740  Product Citations

See how others have used LY 354740. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 26071318  Ma, N. et al. 2015. Clin. Immunol. 160: 142-54.

PMID: # 21451028  Komagata, S. et al. 2011. J. Neurosci. 31: 4896-905.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Orlando Orlando, R. et al. (PubMed 25063582) reported that levels of the Rab GDP dissociation inhibitor (GDI) are altered in the prenatal restrain stress mouse model of schizophrenia and are differentially regulated by the mGlu2/3 receptor agonists, LY 379268 and LY 354740. -SCBT Publication Review
Date published: 2015-02-09
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