SIB 1893A selective antagonist of mGluR-5

SIB 1893 (CAS 6266-99-5)

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Synonym: 2-methyl-6-(2-phenylethenyl)pyridine; [E]-2-Methyl-6-[2-phenylethenyl]pyridine
Application: A selective antagonist of mGluR-5
CAS Number: 6266-99-5
Molecular Weight: 195.26
Molecular Formula: C14H13N
* Refer to Certificate of Analysis for lot specific data (including water content).
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SIB 1893 is a highly selective non-competitive antagonist for the mGluR-5 (metabotropic glutamate receptor 5 type); displays an IC50 value of 0.3 μM at hmGluR-5, compared with > 100 μM at hmGluR-1b, hmGluR-2, hmGluR-6, hmGluR-7 and hmGluR-8.


References

Varney et al (1999) SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J.Pharmacol.Exp.Ther. 290 170. Chapman et al (2000) Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893). Neuropharmacology 39 1567. Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br.J.Pharmacol. 138 1026.

Appearance :
Crystalline
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM). Insoluble in water.
Storage :
Desiccate at 4° C
Melting Point :
43.4-43.9° C
Boiling Point :
307.28° C at 760 mmHg (Predicted)
Density :
1.07 g/cm3 (Predicted)
Refractive Index :
n20D 1.65 (Predicted)
IC50 :
mGluR-5: IC50 = 0.29 µM (human); Glutamate-induced Ca2+ response: IC50 = 0.29 µM (hmGluR5a/L38-20 cells); Quisqualate-induced InsP accumulation: IC50 = 2.3 µM (hmGluR5a/L38-20 cells); Photinus pyralis luciferase: IC50 = 4.3 µM; mGluR-1a: IC50 >100 µM (human)
Ki Data :
mGluR-5: Ki= 0.29 µM (human); mGluR-4: Ki= 26 µM (human); mGluR-7: Ki>100 µM (human); mGluR-2: Ki>100 µM (human); mGluR-6: Ki>100 µM (human)
pK Values :
pKb: 5.42 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UT5810210
PubChem CID :
5311432
MDL Number :
MFCD02262120
SMILES :
CC1=CC=CC(=N1)/C=C/C2=CC=CC=C2

Download SDS (MSDS)

Certificate of Analysis

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