74068-68-1Relevant articles and documents
SINTESI E STUDIO FARMACOLOGICO DI DERIVATI DELL'ORCIPRENALINA E DEL SALBUTAMOLO
Meglio, P. de,Carissimi, M.,Ravenna, F.,Gentili, P.,Manzardo, S.
, p. 202 - 230 (2007/10/02)
The effect of replacing the basic aliphatic residue of orciprenaline and salbutamol with: a) a heterocyclic amine; b) a basic residue containing a phenylcyclohexane radical has been studied.The synthesis of the compounds is outlined.They were tested in vitro for relaxation of histamine-induced spasm of tracheal chains and on the isolated Langendorff heart, and in vivo according to the Konzett and Roessler technique and for their action on the cardiovascular system.In all tests the new derivatives were less active than the reference substances; the only exception was (A) where R = 4-phenylpiperidine (M.G.6604), which was almost as active as orciprenaline in the Konzett and Roessler test, had one third of its activity on isolated trachea and showed absolutely no influence on heart rate in vitro or in vivo.Its effect was not inhibited by β-blocking agents; it therefore showed as antihistaminic profile.