Structure-binding relation of philanthotoxins from nicotinic acetylcholine receptor binding assay.
Philanthotoxins are noncompetitive inhibitors of the nicotinic acetylcholine receptor and the various glutamate receptors. Analogues carrying photoaffinity labels, fluorine atoms for solid-state NMR studies of ligand/receptor interaction, and large head groups such as porphyrins and planar bulky aromatic rings (BIG analogues) for clarifying mode of entry and orientation of analogues in receptors have been synthesized, assayed against the nicotinic acetylcholine receptor, and brief comments are given for the assay results.
Nakanishi
K
K
Department of Chemistry, Columbia University, New York, NY 10027, USA.
Huang
X
X
Jiang
H
H
Liu
Y
Y
Fang
K
K
Huang
D
D
Choi
S K
SK
Katz
E
E
Eldefrawi
M
M
D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D005629:Frozen Sections; D008970:Molecular Weight; D018733:Nicotinic Antagonists / Q000737:chemistry*; D011073:Polyamines; D011166:Porphyrins / Q000737:chemistry; D011978:Receptors, Nicotinic / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014101:Torpedo; D014862:Wasp Venoms / Q000737:chemistry
D000596:Amino Acids; D018733:Nicotinic Antagonists; D011073:Polyamines; D011166:Porphyrins; D011978:Receptors, Nicotinic; D014862:Wasp Venoms; C034092:delta-philanthotoxin