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Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-2-Phenylethyl Ester — JMV180: A Unique CCK Analogue with Different Actions on High- and Low-Affinity CCK Receptors

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Cholecystokinin Antagonists in Gastroenterology

Abstract

During investigations into the structure activity relationships of chole-cystokinin (CCK), it soon became apparent that the C-terminal portion of the CCK molecule, more particularly the C-terminal phenylalanine residue, was of crucial importance for the complete biological activity of CCK analogues, both in the peripheral system and in the CNS. Suppression of the C-terminal phenylalanine residue, e.g., Z-CCK-27–32-NH2 [Z-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-NH2], led to CCK antagonists both in the peripheral system [1] and in the CNS [2,3]. We report here on the modulations in activity which resulted from suppression of the C-terminal primary amide function of CCK, and on its pharmacological consequences.

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Author information

Authors and Affiliations

  1. Facultè de Pharmacie, CCIPE, 15 Av. C. Flahault, 34060, Montpellier Cèdex, France

    P. Fulcrand

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  1. J. Martinez
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  2. M-C. Galas
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  3. M-F. Lignon
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  4. M. Rodriguez
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  5. P. Fulcrand
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Editors and Affiliations

  1. Abteilung Innere Medizin I, Medizinische Klinik und Poliklinik Oberer Eselsberg, Robert-Koch-Straße 8, W-7900, Ulm, Germany

    Guido Adler

  2. Abteilung für Gastroenterologie, Universitätsklinik, Petersgraben 6, 4031, Basel, Switzerland

    Christoph Beglinger

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© 1991 Springer-Verlag Berlin Heidelberg

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Martinez, J., Galas, MC., Lignon, MF., Rodriguez, M., Fulcrand, P. (1991). Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-2-Phenylethyl Ester — JMV180: A Unique CCK Analogue with Different Actions on High- and Low-Affinity CCK Receptors. In: Adler, G., Beglinger, C. (eds) Cholecystokinin Antagonists in Gastroenterology. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-76362-5_9

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  • DOI: https://doi.org/10.1007/978-3-642-76362-5_9

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-76364-9

  • Online ISBN: 978-3-642-76362-5

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