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3-MATIDA

Cat. No. M6338
3-MATIDA Structure
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10mg USD 520  USD520 Custom Synthesis
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Biological Activity

3-MATIDA is a potent metabotropic glutamate mGlu1 receptor antagonist (IC50 = 6.3 μM at rat mGlu1a). Displays ≥ 40-fold selectivity over other receptors: mGlu5, mGlu2, mGlu4a (IC50 > 300 μM), NMDA and AMPA (IC50 = 250 μM). Neuroprotective in cultured murine cortical cells and rat hippocampal slice cultures in vitro. Reduces the volume of ischemia-induced brain infarcts in rats following systemic administration in vivo.

Chemical Information
Molecular Weight 215.23
Formula C8H9NO4S
CAS Number 518357-51-2
Solubility (25°C) 1eq. NaOH 21.52 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Brenton T Laing, et al. AgRP/NPY Neuron Excitability Is Modulated by Metabotropic Glutamate Receptor 1 During Fasting

[2] P M B Cahusac, et al. Non-competitive metabotropic glutamate 1 receptor antagonists block activity of slowly adapting type I mechanoreceptor units in the rat sinus hair follicle

[3] Claudia G Werner, et al. Differential role of mGlu1 and mGlu5 receptors in rat hippocampal slice models of ischemic tolerance

[4] Gabriele Costantino, et al. Stereoselective synthesis and preliminary evaluation of (+)- and (-)-3-methyl-5-carboxy-thien-2-yl-glycine (3-MATIDA): identification of (+)-3-MATIDA as a novel mGluR1 competitive antagonist

[5] Flavio Moroni, et al. The novel and systemically active metabotropic glutamate 1 (mGlu1) receptor antagonist 3-MATIDA reduces post-ischemic neuronal death

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