An orally bioavailable positive allosteric modulator of mGluR4 (EC50 = 1 µM); has a greater than 30-fold selectivity for mGluR4 over mGluR5 in vitro; has no activity at concentrations up to 10 µM at A2A

TCN 238 – 10 mg

Brand:
Cayman
CAS:
125404-04-8
Storage:
-20
UN-No:
Non-Hazardous - /

TCN 238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4; EC50 = 1 µM).{40126} It has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells. It has no activity at the adenosine A2A, serotonin 5-HT1A, or α2A-adrenergic receptors at concentrations up to 10 µM. In a haloperidol-induced catalepsy rat model of Parkinson’s disease, it dose-dependently reduces catalepsy with an ED50 of approximately 1 mg/kg. TCN 238 administration in rats leads to downregulation of the mGluR4 gene, GRM4, in the hippocampus and the gene for the GABAA receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory.{40127}  

 

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Description

An orally bioavailable positive allosteric modulator of mGluR4 (EC50 = 1 µM); has a greater than 30-fold selectivity for mGluR4 over mGluR5 in vitro; has no activity at concentrations up to 10 µM at A2A, 5-HT1A, or α2A-adrenergic receptors; reduces catalepsy in a haloperidol-induced catalepsy rat model of Parkinson’s disease (ED50 = ~1 mg/kg); leads to downregulation of GRM4 and GABRA1 in rat brain without affecting hippocampal-dependent memory

Formal name: (E)-4-(2-phenylethenyl)-2-pyrimidinamine

Synonyms: 

Molecular weight: 197.2

CAS: 125404-04-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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