Article date: November 1974
By: STELLA R. O'DONNELL, JANET C. WANSTALL in Volume 52, Issue 3, pages 407-417
Amines related in structure to either isoprenaline (catechol series) or orciprenaline (resorcinol series) were examined for activity on isolated trachea (relaxation), atria (chronotropic action) and perfused hind‐limb (vasodilatation) of the guinea‐pig.
Compounds with a resorcinol nucleus were less potent on all three preparations but more selective for trachea than were compounds with a catechol nucleus.
In both catechol and resorcinol compounds potency on trachea was enhanced by and selectivity for trachea was favoured by substitution of a p‐OH phenyl group in the N‐isopropyl, or by replacement of the N‐isopropyl with an N‐t‐butyl, with or without a p‐OH phenyl group.
Most of the compounds, particularly the resorcinols, had much lower potencies, relative to isoprenaline, on hind‐limb than on trachea.
Some of the problems associated with the quantitative measurement of selectivity and with sub‐classification of β‐adrenoceptors are discussed.
Amines related in structure to either isoprenaline (catechol series) or orciprenaline (resorcinol series) were examined for activity on isolated trachea (relaxation), atria (chronotropic action) and perfused hind‐limb (vasodilatation) of the guinea‐pig.
Compounds with a resorcinol nucleus were less potent on all three preparations but more selective for trachea than were compounds with a catechol nucleus.
In both catechol and resorcinol compounds potency on trachea was enhanced by and selectivity for trachea was favoured by substitution of a p‐OH phenyl group in the N‐isopropyl, or by replacement of the N‐isopropyl with an N‐t‐butyl, with or without a p‐OH phenyl group.
Most of the compounds, particularly the resorcinols, had much lower potencies, relative to isoprenaline, on hind‐limb than on trachea.
Some of the problems associated with the quantitative measurement of selectivity and with sub‐classification of β‐adrenoceptors are discussed.
DOI: 10.1111/j.1476-5381.1974.tb08610.x
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