Title : Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.

Pub. Date : 2008 Jan 15

PMID : 18078749






1 Functional Relationships(s)
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1 Analogues of the P2X(7) receptor antagonist KN-62, modified at the piperazine and arylsulfonyl groups, were synthesized and assayed at the human P2X(7) receptor for inhibition of BzATP-induced effects, that is, uptake of a fluorescent dye (ethidium bromide) in stably transfected HEK293 cells and IL-1beta release in differentiated THP-1 cells. Piperazine purinergic receptor P2X 7 Homo sapiens