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Distinct functional characteristics of levocabastine sensitive rat neurotensin NT2 receptor expressed in Chinese hamster ovary cells.
- Source :
-
Life sciences [Life Sci] 1998; Vol. 62 (23), pp. PL 375-80. - Publication Year :
- 1998
-
Abstract
- Neurotensin has been shown to produce pharmacological effects both in brain and periphery. Several of these effects are mediated by a high-affinity neurotensin NT1 receptor. On the other hand, a low-affinity levocabastine-sensitive neurotensin NT2 receptor was molecularly cloned from rodent brain recently. In this study, in contrast to NT1 receptor, levocabastine (a histamine H1 receptor antagonist) and SR48692 (an antagonist for NT1 receptor) strongly stimulated intracellular Ca2+ mobilization in transfected Chinese hamster ovary cells expressing rat NT2 receptor, thus acting as potent NT2 receptor. Furthermore, despite of their affinities for NT2 receptor, the Ca2+ responses to potent NT1 agonists, neurotensin or JMV449 ([Lys8-(CH2NH)-Lys9]Pro-Tyr-Ile-Leu, a peptidase resistant analogue of neurotensin) were much smaller than that observed with SR48692. These findings suggest that NT1 and NT2 receptors present distinct functional characteristics and that SR48692 may act as a potent agonist for NT2 receptor.
- Subjects :
- Animals
Calcium metabolism
Cricetinae
Dose-Response Relationship, Drug
Neurotensin pharmacology
Oligopeptides pharmacology
Pyrazoles pharmacology
Quinolines pharmacology
Rats
Receptors, Neurotensin antagonists & inhibitors
Signal Transduction drug effects
Transfection
CHO Cells metabolism
Histamine H1 Antagonists pharmacology
Piperidines pharmacology
Receptors, Neurotensin physiology
Subjects
Details
- Language :
- English
- ISSN :
- 0024-3205
- Volume :
- 62
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Life sciences
- Publication Type :
- Academic Journal
- Accession number :
- 9627096
- Full Text :
- https://doi.org/10.1016/s0024-3205(98)00192-1