11-Deoxy-11α, 12α-methanoprostaglandin E2, a potent, short-acting bronchodilator

Article abstract of DOI:10.1002/jps.2600750322

11-Deoxy-11α,12α-methanoprostaglandin E₂ (1b) and the corresponding methyl ester 7a were highly potent, but short acting, bronchodilators both by the intravenous (80 and 10 times PGE₂, respectively) and aerosol (2 and ~1 times PGE₂) routes, as measured by the Konzett-Rossler assay. The 11β,12β-methano compound 15a was two orders of magnitude less active than 7a. In rhesus monkeys anesthetized by aerosol administration, 1b was 10-50% as potent as, and had a duration of action similar to PGE₁ in the inhibition of methacholine-induced increases in airway resistance. At doses effective in preventing the methacholine response, 1b increased the heart rate (≤ 30%) and precipitated mild upper airway irritation.