Abstract:
:Stable CHO cell clones which selectively express all three rat tachykinin receptors were established by transfection. The binding of radiolabled substance P and neurokinin A (substance K) to CHO clones expressing the NK1 and NK2 receptors, respectively, were saturatable and of high affinity (Kd = 0.17 nM (NK1); 3.4 nM (NK2)). Scatchard analysis of the binding data indicated for both receptors binding to a single population of binding sites, and competition binding studies showed that the binding specificities of the receptors corresponded to those of classical NK1 and NK2 receptors. In contrast, the binding of eledoisin to the NK3 receptor expressed in the transfected CHO cells was of low affinity (IC50 = 240 nM) compared to the high affinity of the receptor found when it was transiently expressed in COS-7 cells (IC50 = 8 nM). However, in both cases the receptor exhibited the specificity of a classical NK3 receptor. The established cell clones may provide an important tool for further analysis of the molecular mechanisms involved in binding, activation, and coupling of receptors for tachykinin peptides.
journal_name
FEBS Lettjournal_title
FEBS lettersauthors
Gether U,Marray T,Schwartz TW,Johansen TEdoi
10.1016/0014-5793(92)80295-rkeywords:
subject
Has Abstractpub_date
1992-01-27 00:00:00pages
241-4issue
3eissn
0014-5793issn
1873-3468pii
0014-5793(92)80295-Rjournal_volume
296pub_type
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