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Eur J Pharm Sci ; 7(1): 29-40, 1998 Dec.
Article in English | MEDLINE | ID: mdl-9845775

ABSTRACT

The synthesis of 3-aralkyl-4-aryl-4H-, 3-aralkylamino-4-aryl-4H- and 3-aralkylsulfanyl-4-aryl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1, 1-dioxides is described. Moreover, the affinity of the different compounds towards the cholecystokinin CCK-A and CCK-B receptors was evaluated. For selected compounds, affinity on the two receptor subtypes was expressed in the micromolar range. This was comparable to the affinity observed with the naturally occurring CCK receptor antagonist asperlicin.


Subject(s)
Receptors, Cholecystokinin/metabolism , Thiadiazines/chemical synthesis , Thiadiazines/metabolism , Animals , Chemical Phenomena , Chemistry, Physical , Kinetics , Ligands , Male , Quinazolines/chemistry , Rats , Rats, Wistar , Receptor, Cholecystokinin A , Receptor, Cholecystokinin B , Sincalide/metabolism , Structure-Activity Relationship , Thiadiazines/pharmacology
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