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- W2094331551 abstract "The existence of two neurokinin NK-3 receptor subtypes has been suggested on the basis of results obtained in binding assays. In the present study, we have confirmed the two NK-3 receptor subtypes by using data obtained in both biological and binding assays. Experiments have been performed in the rat portal vein and in the guinea-pig ileum treated with NK-1 and NK-2 selective antagonists, namely CP 96345 and SR 48968. Orders of potency of agonists on the rat portal vein are as follows: for neurokinins, NKB > NKA > SP; for tachykinins, KAS > ELE > PHY; and for selective agonist: [Mephe7]NKB >> senktide. On the guinea-pig ileum, the agonist rank orders of potency are: NKB > SP > NKA, ELE > KAS > PHY; and for selective agonist: [MePhe7=senktide. The apparent affinity of antagonists shows differences in both biological and binding assays. In fact, on the rat portal vein, SR 48968 is almost inactive (pA2 or IC50 ≈ 4.8), while R-486 [Trp7,βAla8]NKA(4–10) shows a pA2 value of 7.45 and an IC50 of 5.6. An opposite pattern of activity is observed in the guinea-pig ileum, where SR 48968 shows a pA2 of 6.05 and an IC50 of 6.7, while R-486 has a pA2 of 6.1 and an IC50 of < 5.0. These results confirm the existence of two NK-3 sites differing pharmacologically. It is proposed to name NK-3A the receptor of the guinea-pig ileum and NK-3B the receptor of the rat portal vein." @default.
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- W2094331551 title "Two NK-3 receptor subtypes: Demonstration by biological and binding assays" @default.
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- W2094331551 doi "https://doi.org/10.1016/0143-4179(94)90065-5" @default.
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