Histamine H3 receptors regulate acetylcholine release from the guinea pig ileum myenteric plexus

Journal Article · Tue Jan 01 04:00:00 EST 1991 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(91)90531-F· OSTI ID:5924673

Poli, E; Coruzzi, G; Bertaccini, G ^[1]

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1. Univ. of Parma (Italy)

The effect of selective histamine H3-receptor agonists and antagonists on the acetylcholine release from peripheral nerves was evaluated in the guinea pig longitudinal muscle-myenteric plexus preparations, preloaded with ({sup 3}H)choline. In the presence of H1 and H2 blockade, histamine and (R)-{alpha}-methylhistamine inhibited the electrically-evoked acetylcholine release, being (R)-{alpha}-methylhistamine more active than histamine, but behaving as a partial agonist. The effect of histamine was completely reversed by selective H3-blocking drugs, thioperamide and impromidine, while only submaximal doses of (R)-{alpha}-methylhistamine were antagonized. Furthermore, thioperamide and impromidine enhanced the electrically-evoked acetylcholine release. On the contrary, the new H3-blocker, HST-7, was found substantially ineffective, both as histamine antagonist and as acetylcholine overflow enhancer. These data suggest that histamine exerts an inhibitory control on the acetylcholine release from intestinal cholinergic nerves through the activation of H3 receptors.

• OSTI ID: 5924673
• Journal Information: Life Sciences; (USA), Journal Name: Life Sciences; (USA) Vol. 48:13; ISSN 0024-3205; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ACETYLCHOLINE
AMINES
AMMONIUM COMPOUNDS
ANIMALS
ANTIHISTAMINICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZOLES
BIOCHEMICAL REACTION KINETICS
DRUGS
ESTERS
GUINEA PIGS
HETEROCYCLIC COMPOUNDS
HISTAMINE
HYDROGEN COMPOUNDS
IMIDAZOLES
INHIBITION
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MEMBRANE PROTEINS
MUSCLES
NERVES
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PARASYMPATHOMIMETICS
PROTEINS
QUATERNARY COMPOUNDS
REACTION KINETICS
RECEPTORS
RODENTS
SECRETION
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES