Differential agonist activity of somatostatin and L‐362855 at human recombinant sst4 receptors

1 The operational characteristics of somatostatin (SRIF) sst4 receptors are poorly understood. In this study, we have characterized human recombinant sst4 receptors expressed in CHO cells (CHOsst4) by radioligand binding and microphysiometry. 2 Increasing concentrations SRIF or other SRIF receptor l...

Full description

Saved in:
Bibliographic Details
Published in:British journal of pharmacology 1998-10, Vol.125 (4), p.833-841
Main Authors: Smalley, K S M, Feniuk, W, Humphrey, P P A
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Cell receptors
Cell structures and functions
Cells, Cultured
CHO Cells
Cricetinae
desensitization
Dose-Response Relationship, Drug
Fundamental and applied biological sciences. Psychology
Hormone receptors. Growth factor receptors. Cytokine receptors. Prostaglandin receptors
Humans
Hydrogen-Ion Concentration
L‐362855
microphysiometry
Molecular and cellular biology
Neuropeptide receptors
Peptides, Cyclic - antagonists & inhibitors
Peptides, Cyclic - pharmacology
Protein Binding
Radioligand Assay
Receptors, Somatostatin - agonists
Receptors, Somatostatin - antagonists & inhibitors
Recombinant Proteins - drug effects
Somatostatin
Somatostatin - pharmacology
SRIF
sst4 receptors
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:1 The operational characteristics of somatostatin (SRIF) sst4 receptors are poorly understood. In this study, we have characterized human recombinant sst4 receptors expressed in CHO cells (CHOsst4) by radioligand binding and microphysiometry. 2 Increasing concentrations SRIF or other SRIF receptor ligands inhibited specific [125I]‐Tyr11‐SRIF binding in CHOsst4 cell membranes with respective pIC50 values of SRIF (8.82), L‐362855 (7.40), BIM‐23027 (
ISSN:0007-1188
1476-5381
DOI:10.1038/sj.bjp.0702133