Characterization of the muscarinic receptor in isolated uterus of sham operated and ovariectomized rats
| Autor: | G J Stepan, A. Choppin, Richard M. Eglen, Dana N. Loury, N. Watson |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Pharmacology
medicine.medical_specialty Carbachol Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M2 Muscarinic acetylcholine receptor M1 Biology Pirenzepine chemistry.chemical_compound Endocrinology chemistry Himbacine Internal medicine Muscarinic acetylcholine receptor medicine Methoctramine medicine.drug |
| Zdroj: | British Journal of Pharmacology. 127:1551-1558 |
| ISSN: | 0007-1188 |
| DOI: | 10.1038/sj.bjp.0702696 |
| Popis: | The pharmacological characteristics of muscarinic receptors in rat isolated uterus were studied in ovariectomized (ov.) and sham operated (sh.) animals. Competition radioligand binding studies, using uterine membranes and [3H]-NMS, were undertaken with several muscarinic receptor antagonists. Most of the antagonists indicated a one-site fit with apparent affinity estimates (pKi) unchanged by ovariectomy. The selective M2 antagonist, tripitramine revealed high (representing 33±8 and 38±2%) and low (67±8 and 62±2%) affinity binding sites in both sh. and ov. rat uterus, respectively. These sites likely represented muscarinic M2 and M3 receptors and the proportions were not significantly different in the two conditions. Carbachol induced concentration-dependent contractions which were surmountably antagonized by several muscarinic receptor antagonists (pKB, sh.; ov.): zamifenacin (9.19; 9.18), p-F-HHSiD (8.50; 9.06), tripitramine (7.23; 7.54), himbacine (7.21; 7.41), methoctramine (6.79; 7.49), pirenzepine (6.48; 7.21), AF DX 116 (6.26; 6.61), MTx 3 ( |
| Databáze: | OpenAIRE |
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