Aronstam_1985_Biochem.Pharmacol_34_3037

Reference

Title : Binding of [3H]perhydrohistrionicotoxin and [3H]phencyclidine to the nicotinic receptor-ion channel complex of Torpedo electroplax. Inhibition by histrionicotoxins and derivatives - Aronstam_1985_Biochem.Pharmacol_34_3037
Author(s) : Aronstam RS , King CT, Jr. , Albuquerque EX , Daly JW , Feigl DM
Ref : Biochemical Pharmacology , 34 :3037 , 1985
Abstract :

Histrionicotoxin, a spiropiperidine alkaloid, and twenty-two analogs inhibited binding of [3H]perhydrohistrionicotoxin [( 3H]H12-HTX) and of [3H]phencyclidine [( 3H]PCP) to sites on the acetylcholine receptor-ion complex of Torpedo electroplax membranes. Structural alterations to the nitrogen (secondary amine) or oxygen (alcohol) functions or to the five carbon and four carbon side chain of histrionicotoxin altered the potency versus [3H]H12-HTX and [3H]PCP binding measured in the presence or absence of a receptor agonist, carbamylcholine. Histrionicotoxin itself was 3-fold more potent versus [3H]PCP binding than versus [3H]H12-HTX binding. N-Methylation or O-acetylation increased this difference, while alterations to the side chains either slightly decreased or markedly increased this difference. Histrionicotoxin was some 3.5-fold more potent versus [3H]H12-HTX binding in the presence of carbamylcholine than in its absence. O-Acetylation increased this selectivity for the carbamylcholine-activated state of the receptor channel complex, while alterations in the side chains either reduced or increased the selectivity. Histrionicotoxin was some 2.2-fold more potent versus [3H]PCP binding in the presence of carbamylcholine than in its absence. N-Methylation of O-acetyl-histrionicotoxin greatly increased this selectivity, while alterations in the side chains either reduced or had no effect on selectivity.

PubMedSearch : Aronstam_1985_Biochem.Pharmacol_34_3037
PubMedID: 2412560

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Citations formats

Aronstam RS, King CT, Jr., Albuquerque EX, Daly JW, Feigl DM (1985)
Binding of [3H]perhydrohistrionicotoxin and [3H]phencyclidine to the nicotinic receptor-ion channel complex of Torpedo electroplax. Inhibition by histrionicotoxins and derivatives
Biochemical Pharmacology 34 :3037

Aronstam RS, King CT, Jr., Albuquerque EX, Daly JW, Feigl DM (1985)
Biochemical Pharmacology 34 :3037