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ACTIONS OF SOME ANALOGUES OF TRYPTAMINE ON THE ISOLATED RAT UTERUS AND ON THE ISOLATED RAT FUNDUS STRIP PREPARATIONS
Author(s) -
BARLOW R. B.,
KHAN I.
Publication year - 1959
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.1476-5381.1959.tb00934.x
Subject(s) - uterus , fundus (uterus) , tryptamine , gastric fundus , chemistry , pharmacology , endocrinology , medicine , biochemistry , stomach , ophthalmology
Some 3‐(2‐dialkylaminoethyl)‐, 3‐(2‐alkylaminoethyl)‐, and 3‐(2‐dialkylaminoethyl)‐2‐methylindoles have been synthesized and tested, along with 5‐benzyloxygramine, 5‐benzyloxy‐3‐(2‐dimethylaminoethyl)‐, 3‐(2‐aminopropyl)‐ and 3‐(2‐aminobutyl)‐indoles, on the rat uterus and rat fundus strip. 5‐Benzyloxy‐3‐(2‐dimethylaminoethyl)indole, even though it contains an ethylene side‐chain, was a less potent antagonist of 5‐hydroxytryptamine than was 5‐benzyloxygramine. The remaining compounds were still less active. There are differences between the ability of some of them to antagonize 5‐hydroxytryptamine and to antagonize tryptamine. 3‐(2‐Dimethylaminoethyl)‐2‐methylindole, in particular, shows a considerable degree of specific antagonism of 5‐hydroxytryptamine on both tissues. Nearly all the compounds stimulate the preparations, some combining antagonism of 5‐hydroxytryptamine at low concentrations with stimulant activity at higher concentrations. The most active compound is 3‐(2‐dipropylaminoethyl)indole. On the rat fundus strip this has, on a molar basis, 1/40th of the stimulant activity of 5‐hydroxytryptamine, and is 20 times as active as tryptamine: on the rat uterus it is only 1/200th as active as 5‐hydroxytryptamine, and equal in activity to tryptamine.