Abstract |
[125I] Cholecystokinin-8-S (CCK-8-S) bound to a single class of saturable binding sites on the human neuroblastoma cell line IMR-32 (KD = 4 +/- 1.5 nM, Bmax = 10,500 +/- 3,500 sites/cell (n = 6)). These binding sites were of the CCKA type, as demonstrated by the differential inhibition of the binding of [125I]CCK-8-S and CCK-8-S-induced 45Ca2+ efflux by the specific CCKA antagonist SR 27897 and the specific CCKB antagonist PD 134,308. CCK-JMV-180, an analogue of CCK-8-S which has been shown to activate 45Ca2+ efflux in rat cells in a manner similar to CCK-8-S, acted as a potent antagonist of CCK-8-S-induced 45Ca2+ efflux (IC50 = 50 nM) and inhibited [125I]CCK-8-S binding to IMR-32 cells (IC50 = 1.7 nM). These results show that, unlike its CCK-like effect in various animal systems, CCK-JMC-180 acts as an antagonist of CCKA receptors in the human neuroblastoma cell line IMR-32.
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Authors | P Schaeffer, V Prabonnaud, M Roux, D Gully, J M Herbert |
Journal | FEBS letters
(FEBS Lett)
Vol. 354
Issue 2
Pg. 203-6
(Nov 07 1994)
ISSN: 0014-5793 [Print] England |
PMID | 7957924
(Publication Type: Journal Article)
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Chemical References |
- Calcium Radioisotopes
- Receptors, Cholecystokinin
- JMV 180
- Sincalide
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Topics |
- Calcium Radioisotopes
(metabolism)
- Humans
- Kinetics
- Neuroblastoma
(metabolism)
- Receptors, Cholecystokinin
(antagonists & inhibitors, metabolism)
- Sincalide
(analogs & derivatives, metabolism, pharmacology)
- Tumor Cells, Cultured
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