Binding of Acetylcholine Receptor/Channel Probes to Housefly Head Membranes

Eldefrawi, Amira T.; Shaker, N.; Eldefrawi, Mohyee E.

doi:10.1002/9780470720707.ch10

Cited by 4 publications

References 27 publications

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Structure-activity relationships of acyclic nicotinoids and neonicotinoids for insect nicotinic acetylcholine receptor/ion channel complex

Matsuo

Tomizawa

Yamamoto

1998

Arch. Insect Biochem. Physiol.

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The insect nicotinic acetylcholine (Ach) receptor (nAChR) is a target site for the neonicotinoid insecticides such as imidacloprid and its acyclic derivative acetamiprid. The structure–activity relationships of acetamiprid homologues and 3‐pyridylmethylamines (known as the essential structural requirement of nicotinoid) are compared in terms of the affinity to the [3H]α‐bungarotoxin (α‐BGT) site (designated as Ach site) and the [3H]phencyclidine (PCP) site [designated as noncompetitive blocker (NCB) site] of the insect nAChR from the honeybee heads. Increasing the chain length of alkyl substituents (from methyl to n‐butyl) on an amino nitrogen atom of acetamiprid homologue and 3‐pyridylmethylamine reduces the potency as inhibitors of [3H]α‐BGT binding, whereas it confers the enhanced potency as inhibitors of [3H]PCP binding in the insect nAChR. Scatchard analysis reveals that homologues of acetamiprid and 3‐pyridylmethylamine having n‐butyl substituents interact with the high‐affinity binding site for [3H]PCP, which is considered to be the NCB site located in the ion channel of the insect nAChR. The interaction of acetamiprid homologues with the Ach or NCB site of nAChR is selective for insects, while that of the 3‐pyridylmethylamines is effective for both insect and Torpedo [Tomizawa et al., J Pesticide Sci 21:412–418 (1996)]. The explorations in further structural modification of neonicotinoid compounds may facilitate development of new insecticides or probes for the ion channel of insect nAChR. Arch. Insect Biochem. Physiol. 37:17–23, 1998. © 1998 Wiley‐Liss, Inc.

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Structure-activity relationships of acyclic nicotinoids and neonicotinoids for insect nicotinic acetylcholine receptor/ion channel complex

Matsuo

Tomizawa

Yamamoto

1998

Arch. Insect Biochem. Physiol.

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Binding of [³H]phencyclidine to membranes from housefly thoracic muscles

Filbin

Eldefrawi

1985

Arch Insect Biochem Physiol

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The drug binds to sites in the mammalian brain, and this binding correlates fairly well with its behavioral effects [3,4]. PCP* also binds to and affects the function of vertebrate skeletal [5] and smooth [6] muscles. It has two effects on the skeletal muscle. It inhibits the nicotinic ACh receptor in the motor end plate noncompetitively, by binding to its channel sites, and it inhibits the voltage-dependent outward rectifier K+ channels of the muscle membrane *Abbreviations: ACh = acetylcholine; IC50 = drug concentration that inhibits 50% of binding; Ki = inhibition constant; LDS0 = dose that kills 50%; PCP = phencyclidine.Acknowledgments: We are grateful to Dr. David Triggle for providing us with the Ca2+

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