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EFFECT OF CHAIN LENGTH OF ALIPHATIC AMINES ON HISTAMINE POTENTIATION AND RELEASE
Author(s) -
MONGAR J. L.
Publication year - 1957
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1957.tb00112.x
Subject(s) - histamine , chemistry , intracellular , contractility , biophysics , biochemistry , stereochemistry , chromatography , pharmacology , endocrinology , biology
Diamines in the series NH a .(CH 2 ) n .NH 2 specifically potentiate histamine contractions of the guinea‐pig ileum and inhibit the enzymatic destruction of histamine. These activities are greatest with short‐chain compounds (n⋍5). Diamines also release histamine from isolated tissues and depress the contractility of plain muscle and the motility of paramecia. These activities increase with chain‐length and are probably limited only by solubility. The parallelism between histamine‐releasing activity and toxicity also extends to the monoamines in the series CH 3 .(CH 2 ) n‐1 .NH 2 . Histamine‐releasing activity of both series increases with increase of p H and can mainly be attributed to the non‐ionized base. From the results on the effect of chain‐length and ionization on activity, it is suggested that aliphatic amines release histamine by penetration of the cell membrane in the non‐ionized form, followed by exchange in the ionic form with intracellular histamine.