Preparation and characterization of a probe for the cholecystokinin octapeptide receptor, N/sup. cap alpha. / (/sup 125/I-desaminotyrosyl)CCK-8, and its interactions with pancreatic acini

Journal Article · Thu Dec 10 04:00:00 EST 1981 · J. Biol. Chem.; (United States)

OSTI ID:5632363

Miller, L J; Rosenzweig, S A; Jamieson, J D

A biologically active, high specific activity (2000 Ci/mmol), radiolabeled derivative of cholecystokinin octapeptide (CCK-8) was synthesized, purified, characterized, and used to investigate interactions between CCK-8 and its receptor on rat pancreatic acini. N/sup ..cap alpha../(/sup 125/I-desaminotyrosyl)CCK-8 was prepared by acylation of CCK-8 with /sup 125/I-labeled N-hydroxysuccinimidyl 3-(4-hydroxyphenyl)propionate in dimethylformamide and triethylamine. It was purified by cation exchange chromatography (sulfopropyl-Sephadex), followed by either gel filtration on Sephadex G-25 or high performance liquid chromatography on a reversed-phase C-18 column. Its nonradioactive analogue, N/sup ..cap alpha../(/sup 125/I-desaminotyrosyl)CCK-8 to pancreatic acini was rapid, reversible, temperature-dependent, saturable, and specific. This binding was inhibited by each molecular species of cholecystokinin, but not by structurally unrelated ligands. Good correlation existed between potencies of the species of cholecystokinin for inhibiting binding of this receptor probe and for stimulating pancreatic secretion. N/sup ..cap alpha../(/sup 125/I-desaminotyrosyl) CCK-8 binding was inhibited by its nonradioactive analogue, N/sup ..cap alpha../(/sup 127/I-desaminotyrosyl)CCK-8, in a manner identical with that by iodinated desaminotyrosyl moiety to the NH/sub 2/-terminal end of CCK-8 does not compromise the ability of this peptide to either bind to its pancreatic receptor or stimulate a biologic response.

• Research Organization: Yale Univ. School of Medicine, New Haven, CT
• OSTI ID: 5632363
• Journal Information: J. Biol. Chem.; (United States), Journal Name: J. Biol. Chem.; (United States) Vol. 256:23; ISSN JBCHA
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOLOGICAL FUNCTIONS
BODY
CHEMICAL ANALYSIS
CHEMICAL PREPARATION
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
FUNCTIONS
GLANDS
HORMONES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
MAMMALS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PANCREAS
PEPTIDES
POLYPEPTIDES
PROTEINS
QUANTITATIVE CHEMICAL ANALYSIS
RADIOASSAY
RADIOIMMUNOASSAY
RADIOISOTOPES
RATS
RECEPTORS
RODENTS
SYNTHESIS
TEMPERATURE DEPENDENCE
TRACER TECHNIQUES
UPTAKE
VERTEBRATES