Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
[3H]SR 48968, a radiolabeled nonpeptide antagonist of NK-2 receptor, has been tested in ligand-receptor binding assays using rat duodenum, hamster urinary bladder and guinea pig ileum membranes. [3H]SR 48968 bound to a single class of high affinity binding sites. Its affinity was slightly species-dependent. Its binding was inhibited by neurokinins, following the rank order of potency NKA > NKB > SP. It was also inhibited by peptide antagonists of NK-2 receptor (MEN 10,376, L 659,877), but their relative potencies were highly species-dependent. Unlabeled SR 48968, but not its R-enantiomer (SR 48965), also potently inhibited its binding. These data show that [3H]SR 48968 potently binds to NK-2 receptor and therefore is a useful tool to study NK-2 receptor.
Emonds-Alt
X
X
Sanofi Recherche, Montpellier, France.
Golliot
F
F
Pointeau
P
P
Le Fur
G
G
Breliere
J C
JC
D000818:Animals; D001549:Benzamides / Q000378:metabolism*; D001665:Binding Sites; D001667:Binding, Competitive; D006224:Cricetinae; D004386:Duodenum / Q000378:metabolism; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007700:Kinetics; D008647:Mesocricetus; D010880:Piperidines / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013373:Substance P / Q000037:antagonists & inhibitors*; D001743:Urinary Bladder / Q000378:metabolism
D001549:Benzamides; D010880:Piperidines; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter; D013373:Substance P; C073839:SR 48968