Compared Activities of some Cl- Channel Blockers

	ION CHANNEL and RECEPTOR LIGANDS TOXINS & ALKALOIDS Compared Activities of some Cl ^- Channel Blockers

PRODUCT	Cl- channel blockade [IC₁₀₀] Lymnaea stagnalis	GABA-dependent ³⁵Cl^--uptake blockade [IC₅₀] rat synaptosomes	GABA-dependent Cl^- current blockade [IC ₁₀₀]	[³H]-dihydro- picrotoxin binding inhibition [IC₅₀] P ₂ membrane fraction rat brain	[³⁵S]-TBPS binding inhibition [IC₅₀] P ₂ membrane fraction rat brain	Toxicity (LD₅₀) mice i.p. (mg/kg)
MEBICYPHAT	0.5 然		642 然	150 然	100 然	32
ETBICYPHAT	0.05 然			5.0 然	5.9 然	1
ISOBICYPHAT		0.2 nM	2.75 然	8.0 然	0.48 然	0.18
PROPYBICYPHAT		0.5 nM	1.09 nM	8.0 然	1.1 然	0.38
ETBICYTHIONAT		0.2 nM			3.2 然 (house fly)	1.1
TETS					0.5 然	0.24
CLOFLUBICYNE		10 nM	5.32 nM			0.1
FLUCYBENE		50 nM	61 nM			1.0

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