Description
KF 17837S is an adenosine A(2a) receptor antagonists, which is potential therapeutic and neuroprotective effects in Parkinson's disease.
in vitro
The novel A2A receptor antagonist, (E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine (KF 17837), blocked the CGS 21680 (1 nM)-induced inhibition of [3H]-GABA efflux with an EC50 of approximately 30 nM and also antagonized the CGS 21680 (0.1 nM)-induced stimulation of [3H]-ACh release with an EC50 of approximately 0.3 nM._x000D_
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Reference: Br J Pharmacol. 1994 Sep;113(1):43-8. https://pubmed.ncbi.nlm.nih.gov/7812630/
in vivo
Autoradiographic study of [3H]KF17837S binding using rat brain sections revealed that the binding site was highly enriched in the striatal region. These data indicate that [3H] KF17837S labels the adenosine A2A receptor in rat brain._x000D_
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Reference: Mol Pharmacol. 1994 Nov;46(5):817-22. https://pubmed.ncbi.nlm.nih.gov/7969067/
target
KF 17837S is an adenosine A(2a) receptor antagonists.