(/sup 3/H) Boc (Nle/sup 28,31/)CCK/sub 27-33/, a new highly labelled ligand for CCK receptors: binding on brain and on pancreas

Journal Article · Mon Dec 30 04:00:00 EST 1985 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(85)90605-8· OSTI ID:6301378

Pelaprat, D; Zajac, J M; Gacel, G; Durieux, C; Morgat, J L; Sasaki, A; Roques, B P

Preliminary results on the binding of (/sup 3/H)Boc(Nle/sup 28,31/)CCK/sub 27-33/, designated (/sup 3/H)Boc(diNle)CCK/sub 7/, on mouse brain and rat pancreas membranes are presented. This new ligand for CCK receptors possesses a high specific activity (144 Ci/mmole), and binds in a saturable manner to mouse brain (Kd = 0.49 nM, Bmax = 49 fmoles/mg protein) and rat pancreas (Kd = 4.4 nM, Bmax = 696 fmoles/mg protein). Unlabelled Boc(diNle)CCK/sub 7/ displaces (/sup 125/I)CCK/sub 8/ from its binding sites on mouse brain membranes with a high affinity, slightly superior to that of CCK/sub 8/. The order of potencies to displace (/sup 3/H)Boc(diNle)CCK/sub 7/ from its binding sites was the same in mouse brain and rat pancreas: (/sup 3/H)Boc(diNle)CCK/sub 7/ > CCK/sub 8/, Boc-CCK/sub 7/ > non-sulfated CCK/sub 8/, the pancreas binding sites being more discriminative than the brain binding sites. Thus (/sup 3/H)Boc(diNle)CCK/sub 7/ is a very promising new probe for the characterization of CCK receptors and their interaction with different CCK fragments. 20 references, 4 figures, 1 table.

• Research Organization: CNRS, Paris, France
• OSTI ID: 6301378
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 37:26; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CELL CONSTITUENTS
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM
COMPARATIVE EVALUATIONS
DATA
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
EXPERIMENTAL DATA
GLANDS
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MEMBRANES
MICE
NERVOUS SYSTEM
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PANCREAS
PEPTIDES
POLYPEPTIDES
PROTEINS
RADIOISOTOPES
RATS
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES