Two NK-3 receptor subtypes: demonstration by biological and binding assays

Neuropeptides
Q T NguyenD Regoli

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]NKB = 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 approximately 4.8), while R-486 [Trp7, beta Ala8]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 tw...Continue Reading

References

May 15, 1992·Biochemical and Biophysical Research Communications·C AdvenierD Regoli
Jul 1, 1987·Neuropeptides·G DrapeauD Regoli
Apr 1, 1981·Canadian Journal of Physiology and Pharmacology·P GaudreauD Regoli
Feb 26, 1993·Biochemical and Biophysical Research Communications·F PetitetJ Glowinski
Apr 1, 1964·British Journal of Pharmacology and Chemotherapy·H P RANG

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Citations

Jan 1, 1994·Life Sciences·D RegoliD Jukic
May 4, 1995·Regulatory Peptides·U Holzer-Petsche
Sep 1, 1995·General Pharmacology·C A Maggi
Jan 29, 1997·European Journal of Pharmacology·J C BeaujouanJ Glowinski
Jan 1, 1997·British Journal of Pharmacology·A D MedhurstD W Hay
Dec 19, 2013·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Catherine Belzung
Jun 28, 2008·Neuropeptides·Frankie H M ChengJohn A Rudd

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