Characterization of 125I-Trp11-Neurotensin Binding to Rat Fundus Smooth Muscle Plasma Membranes
The brain-gastrointestinal tridecapeptide neurotensin (NT) has been shown to affect the contractility of a variety of gastrointestinal smooth muscle preparations in vitro . In particular, it has been reported that NT contracts rat fundus smooth muscle strips . Rharmacological experiments and structure activity studies have suggested that this effect was myogenic in nature and involved an interaction of NT with specific smooth muscle receptors . In the present paper we provide direct evidence for the existence of such receptors from radioligand binding studies using 125I-Trp11-NT as the labelled ligand and highly purified rat fundus smooth muscle plasma membranes at the source of NT receptors.
KeywordsGastrointestinal Motility High Affinity Binding Site Radioligand Binding Study Structure Activity Study Label Ligand
Unable to display preview. Download preview PDF.
- 4.Mazella, J., Poustis, C., Labbé, C., Checler, F., Kitabgi, P., Granier, C., Van Rietschoten, J. and Vincent, J.P. (1983). Monoiodo-(Trp11)-neurotensin, a highly radioactive ligand of neurotensin receptors. Preparation, biological activity, and binding properties to rat brain synaptic membranes. J. Biol. Chem., 258, 3476–3481PubMedGoogle Scholar
- 5.Kwan, C.Y., Sakai, Y., Grover, A.K. and Lee, R.M. K.W. (1982). Isolation and characterization of plasma membrane fraction from gastric fundus smooth muscle of the rat. Mol. Physiol., 2, 107–120Google Scholar
- 6.Quirion, R., Regoli, D., Rioux, F. and St Pierre, S. (1980). Structure activity studies with neurotensin ana-lysis in positions 9, 10 and 11. Br. J. Pharmacol., 69, 698–692Google Scholar