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under licence granted by the University of Pennsylvania
Biological Activity:
A high affinity inhibitor for
inward-rectifier K+ channels, this compound is a stable derivative
of the bee venom toxin tertiapin. Binds to ROMK1 (KIR1.1) and
GIRK1/4 (KIR3.1/3.4) channels with high affinity (Ki
values are 1.3 and 13.3 nM respectively) and is selective over IRK1 channels.
Jin and Lu (1999) Synthesis of a stable form of tertiapin: a
high-affinity inhibitor for inward-rectifier K+ channels.
Biochemistry 38 14286. Jinet al (1999) Mechanisms
of inward-rectifier K+ channel inhibition by tertiapin-Q.
Biochemistry 38 14294.
“Tocris is to be congratulated for continuing to meet the current demand for a rapid and reliable source of high-quality compounds that are urgently needed as pharmacological tools by a growing international population of cannabinoid researchers..”
