Marker for growth hormone-releasing factor receptors

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/60 (2006.01) A23K 1/165 (2006.01) A61K 38/25 (2006.01) C07K 16/26 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2158782

The present invention relates to a compound having the formula: Ra-X-Rb I or a pharmaceutically acceptable salt thereof, wherein, X is selected from the group consisting of (see formula II), (see formula III), (see formula IV), (see formula V) and CH2; Ra is a fluorophore selected from the group consisting of fluorescein, rhodamine, Texas red, BODIPY.TM., Cascade blue, coumarin, phycoerithryn, eosin, rosamine and the fluorenyl moiety; and Rb is a polypeptide moiety for binding to GRF receptors which allows for receptor physiological studies in vivo or in vitro and for distinguishing cell surface from intracellular receptor components. The present invention also relates to a method for the labeling of GRF receptors on cell surface.

La présente invention concerne un composé ayant la formule suivante : Ra-X-Rb I ou un sel pharmaceutiquement acceptable de celui-ci, dans laquelle X est choisi parmi le groupe constitué de (voir formule II), (voir formule III), (voir formule IV), (voir formule V) et CH2; Ra est un fluorophore choisi parmi le groupe constitué de fluorescéine, de rhodamine, de rouge Texas, de BODIPY.TM, de bleu cascade, de coumarine, de phycoerithryn rosamine, d'éosine et de fraction fluorényle; et Rb est une fraction de polypeptide pour une liaison à des récepteurs GRF, ce qui permet des études physiologiques de récepteur in vivo ou in vitro et la distinction de la surface cellulaire des composants récepteurs intracellulaires. La présente invention concerne également un procédé de marquage de récepteurs GRF sur une surface cellulaire.

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