Blockers for excitatory effects of achatin-I, a tetrapeptide having a D-phenylalanine residue, on a snail neurone.

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Santos DE, Liu GJ, Takeuchi H

Blockers for excitatory effects of achatin-I, a tetrapeptide having a D-phenylalanine residue, on a snail neurone.

Eur J Pharmacol. 1995 Jan 16;272(2-3):231-9.

PubMed ID

7713167 [ View in PubMed

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Abstract

Some histamine H1 receptor antagonists suppressed the inward current (Iin) of an Achatina identifiable neurone type, PON (periodically oscillating neurone), caused by an Achatina endogenous tetrapeptide having a D-phenylalanine residue, achatin-I (Gly-D-Phe-Ala-Asp), under voltage clamp. Achatin-I was applied locally to the neurone by brief pneumatic pressure ejection and antagonists were administered by perfusion. The dose-response curves of the effective histamine H1 antagonists indicated their potency order to suppress the Iin as follows: chlorcyclizine, promethazine, triprolidine and homochlorcyclizine > trimeprazine and clemastine > diphenylpyraline. The potent drugs were mostly piperazine and phenothiazine types. The effects of chlorcyclizine, promethazine and triprolidine on the dose (the duration of the pressure ejection)-response curve of achatin-I indicated that these drugs affected the Iin caused by achatin-I in a non-competitive manner. The antagonists for the receptors of the small-molecule neurotransmitters other than histamine H1, such as histamine H2, acetylcholine, gamma-aminobutyric acid (GABA), L-glutamic acid, dopamine, alpha- and beta-adrenalin and 5-hydroxytryptamine, had no effect on the Iin caused by achatin-I.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Alimemazine	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details