1973
DOI: 10.1111/j.2042-7158.1973.tb10048.x
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Antibronchoconstrictor activity of two new phosphodiesterase inhibitors, a triazolopyrazine (ICI 58 301) and a triazolopyrimidine (ICI 63 197)

Abstract: A triazolopyrazine (ICI 58 301) and a triazolopyrimidine (ICI 63 197), both potent inhibitors of 3'5'-cyclic adenosine monophosphate phosphodiesterase, protected conscious guinea-pigs against an otherwise lethal bronchospasm caused by inhalation of histamine. Both compounds were active when given by mouth and the activity was both rapid in onset and persistent. Bronchospasm caused by histamine or acetylcholine in guinea-pig isolated lungs was reduced when the lungs were perfused with dilute solutions of the co… Show more

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Cited by 30 publications
(11 citation statements)
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“…The blockade of 5' AMP has also been seen by Phillis & Kostopoulos (1975). It (Davies, 1973) causing, on balance, a reduction of acetylcholine responses.…”
Section: Discussionmentioning
confidence: 74%
“…The blockade of 5' AMP has also been seen by Phillis & Kostopoulos (1975). It (Davies, 1973) causing, on balance, a reduction of acetylcholine responses.…”
Section: Discussionmentioning
confidence: 74%
“…Triazolopyridine is a pyridine com pound similar to dipyridamole that was originally studied as a phosphodiesterase inhibitor and bronchodilator [189]. It was eventually marketed as a smooth muscle vasodilator and antianginal agent in Japan.…”
Section: Antiproliferative Drugsmentioning
confidence: 99%
“…These results imply that the functional antagonists could not fully overcome a cholinergic component in the disease. As well, the future may see the development of potent phosphodiesterase inhibitors, such as ICI 58301 [72] or flavanoid compounds [73] for use in asthma therapy. Even very recent discoveries such as reproterol, a molecular combination of a phenylethylamine derivative and theophylline may play a role in specific asthma therapy to the demise of the established older medications (personal communication -Professor Dr W. Schumtzler, Aachen, FRG).…”
Section: Discussionmentioning
confidence: 99%