Rd. Pinnock et al., CHARACTERIZATION OF TACHYKININ MEDIATED INCREASES IN [CA2-HAMSTER OVARY CELLS EXPRESSING HUMAN TACHYKININ NK3 RECEPTORS(](I) IN CHINESE), European journal of pharmacology. Molecular pharmacology section, 269(1), 1994, pp. 73-78
The nature of the senktide response of the human NK3 receptor expresse
d in Chinese hamster ovary cells was characterised using the Ca2+ sens
itive dye Fura-2 and imaging methods. Application of the NK3 receptor
agonist senktide caused an increase in [Ca2+](i) in the cells. The pro
file for NK3 receptor agonists was that senktide was more potent than
[beta-Ala(8)]neurokinin A-(4-10) which was more potent than [Sar(9),Me
t(O-2)(11)]substance P. SR 48968 was a poor antagonist of the senktide
response in intact cells confirming the weak affinity of this agent f
or the NK3 receptor (IC50 of similar to 1 mu M) shown in binding assay
s. The NK3 receptor mediated increase in intracellular Ca2+ was indepe
ndent of [Ca2+](o), blocked by the microsomal Ca2+ ATPase inhibitor th
apsigargin and the phospholipase C inhibitor U73122 but not by ryanodi
ne. Thus the source of the Ca2+ was probably a ryanodine insensitive,
inositol triphosphate sensitive intracellular store.