Activities of calcitonin gene-related peptide (CGRP) and related peptides at the CGRP receptor

Journal Article · Tue May 01 00:00:00 EDT 1990 · Peptides (Fayetteville, New York); (USA)

DOI:https://doi.org/10.1016/0196-9781(90)90047-9· OSTI ID:6532080

Maton, P N; Pradhan, T; Zhou, Z C; Gardner, J D; Jensen, R T ^[1]

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1. National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, MD (USA)

In guinea pig pancreatic acini rat calcitonin gene-related peptide (CGRP) increased amylase release 2-fold, salmon calcitonin had an efficacy of only 44% of that of CGRP and (Tyr0)CGRP(28-37) and human calcitonin had no actions. (Tyr0)CGRP(28-37), but not human calcitonin, antagonized the actions of CGRP in pancreatic acini with an IC50 of 3 microM. (Tyr0)CGRP(28-37) produced a parallel rightward shift in the dose-response curve for CGRP-stimulated amylase secretion. The inhibition was specific for CGRP and was reversible. Studies with 125I-CGRP demonstrated that CGRP, salmon calcitonin and (Tyr0)CGRP, but not human calcitonin, interacted with CGRP receptors on pancreatic acini. These results indicate that various CGRP-related peptides demonstrate different relationships between their abilities to occupy the CGRP receptor and to affect biologic activity, with CGRP itself being a full agonist, salmon calcitonin a partial agonist, (Tyr0)CGRP(28-37) a competitive antagonist, and human calcitonin having no actions.

• OSTI ID: 6532080
• Journal Information: Peptides (Fayetteville, New York); (USA), Journal Name: Peptides (Fayetteville, New York); (USA) Vol. 11:3; ISSN PPTDD; ISSN 0196-9781
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINO ACID SEQUENCE
AMYLASE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
CALCITONIN
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
DOSE-RESPONSE RELATIONSHIPS
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
ENZYMES
GENES
GLANDS
GLYCOSYL HYDROLASES
GUINEA PIGS
HORMONES
HYDROLASES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
MAMMALS
MAN
MEMBRANE PROTEINS
MOLECULAR STRUCTURE
NUCLEI
O-GLYCOSYL HYDROLASES
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PANCREAS
PEPTIDE HORMONES
PEPTIDES
POLYPEPTIDES
PRIMATES
PROTEINS
RADIOISOTOPES
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SECRETION
TRACER TECHNIQUES
VERTEBRATES