Investigation of behavioral and electrophysiological responses induced by selective stimulation of CCKB receptors by using a new highly potent CCK analog, BC 264
✍ Scribed by V. Dauge; G. A. Bohme; J. N. Crawley; C. Durieux; J. M. Stutzmann; J. Feger; J. C. Blanchard; B. P. Roques
- Book ID
- 104600336
- Publisher
- John Wiley and Sons
- Year
- 1990
- Tongue
- English
- Weight
- 926 KB
- Volume
- 6
- Category
- Article
- ISSN
- 0887-4476
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✦ Synopsis
The new CCKB analog, Boc-Tyr (S0,H)-gNle-mGly-Trp-(NMe)-Nle-Asp-PheNHJBC 264) exhibited a high affinity (KI = 0.39 2 0.15 nM) and selectivity for central (B) versus peripheral (A) receptors (KI CCKAKI CCKB = 910) in the rat. In agreement with these binding studies, BC 264 was a t least 50 times more potent than CCK, in stimulating the firing of rat CA hippocampal neurones. Furthermore stereotaxic injection of BC 264 or CCK, in the VTA of rats resulted in potentiation of the dopamineinduced hypolocomotion. These two types of CCK, responses have been previously shown to involve CCKB receptors. In contrast, after administration into the postero-median nucleus accumbens, the hypoexploration, the increase of emotionality of rats, or the potentiation of dopamine-induced hyperlocomotion were obtained after injection of CCK, but not of BC 264, supporting the involvement of peripheral CCKA receptors in these CCK, responses. Owing to its resistance to peptidases, BC 264 appears to be of great interest in the investigation of the still uncertain functional roles of CCK in the central nervous system.