NK1 and NK2 receptors are similar in man and rabbit.
A series of 15-18 compounds that act on NK1 or NK2 receptors as agonists or antagonists have been tested in the monoreceptor systems of the rabbit vena cava (NK1) and the rabbit pulmonary artery (NK2) for biological activities and for their ability to displace [3H] [Sar9, Met(O2)11]SP or [125I] NKA respectively from NK1 or NK2 human binding sites obtained by transfection and functional expression of the cDNAs for these receptor subtypes in CHO-K1 cells. For the two tachykinin receptors studied, positive highly significant correlations have been shown between binding and biological assays. Slopes of correlations are linear and near unity (r = 0.918 and 0.938). For NK1 and NK2 receptors the pharmacology in human and rabbit tissues appears to be very similar. The assays of biological activity on rabbit tissues may be therefore used to complement binding studies on human transfected cells to identify new antagonists for human tachykinin receptors.
Coge
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F
Département de Biologie Cellulaire et Moléculaire, Institut de Recherche Servier, Suresnes, France.
Regoli
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D
D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D007457:Iodine Radioisotopes; D007700:Kinetics; D009131:Muscle, Smooth, Vascular / Q000378:metabolism*; D015288:Neurokinin A / Q000378:metabolism; D011651:Pulmonary Artery / Q000378:metabolism*; D011817:Rabbits; D018040:Receptors, Neurokinin-1 / Q000378:metabolism*; D018041:Receptors, Neurokinin-2 / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D013373:Substance P / Q000031:analogs & derivatives / Q000378:metabolism; D014162:Transfection; D014316:Tritium; D014684:Venae Cavae / Q000378:metabolism*
D007457:Iodine Radioisotopes; D018040:Receptors, Neurokinin-1; D018041:Receptors, Neurokinin-2; D011994:Recombinant Proteins; D014316:Tritium; C062618:substance P, Sar(9)-Met(O2)(11)-; D013373:Substance P; D015288:Neurokinin A