Pharmacological Studies of Trimetoquinol Analocs As Antiaccrecatory And Cardiopulmonary Drugs

TMO, the prototype drug for these studies is reported to possess significant Ilogical activities at 2- 1- and 2-adrenoceptor properties (Feller etal.;Soberet 211.,1981; Lee et al., 1974; Mayo et al.,1981; Mukhopadhyay et al.,i2);and to exhibit potent anti- TXA2 actions in platelets and vasculature (Mayo et\98\; Mukhopadhyay et al., 1985). 5-FTMQ and 8-FTMQ have been synthesized to sthe role of fluorine atom substitution on the aromatic ring of TMQ, and were Iluated for 1- andPGH2 antagonist activities in rat thoracic aorta and human platelets; and for comparative antiaggregatory and secretory effects against iglandin-dependent and -independent pathways of platelet activation. Fluorine atom substitution of TMQ at the 5- or 8-pd the potent ~2-agonist propert ies in trachea, but had great ly reduced agonist tyagainst ~ l-adrenoceptors in guinea pig right atria (cbronotropy) and ’,cally- driven left atria (inotropy). Each compound either produced positive Itropic effects in spont