β1 and β2 Stimulatory effects of prenalterol
Mattsson, H. ; Andersson, T. ; Carlsson, E. ; Hedberg, A. ; Lundgren, B. ; Olsson, T.
Springer
Published 1982
Springer
Published 1982
| ISSN: |
1432-1912
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|---|---|
| Keywords: |
Prenalterol ; Agonistic acitivity ; β-Adrenoceptors ; Spare receptors ; Cyclic AMP
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| Source: |
Springer Online Journal Archives 1860-2000
|
| Topics: |
Medicine
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| Notes: |
Summary Prenalterol, previously characterized as a functionally cardioselective partial β-adrenoceptor agonist, was shown to relax K+-elicited contractures in the uterine muscle from progesterone pretreated rats (pD 2 7.7) and to increase beating rate in the rat right atrium (pD 2 8.0) at about the same concentrations with maximal effects corresponding to 94 and 82% respectively of those of isoproterenol. Terbutaline, with equal maximal effects as isoproterenol, was 50 times more potent in the uterus (pD 2 7.8) than in the right atrium (pD 2 6.1). Both tissues displayed a high sensitivity to isoproterenol (pD 2 9.1 in both tisues) indicating large receptor reserves for the full agonist. The maximal relaxing effect of prenalterol in the uterus was obtained at about a three-fold increase of the cyclic AMP content, which is similar to that obtained with isoproterenol at a corresponding relaxation. The effects in the uterine muscle of all three agonists were mediated through β2-adrenoceptors since β2-adrenoceptor blockers (ICI 118,551 and IPS 339) antagonized the effects in concentrations which had only marginal effects on the atrial responses of the agonists. The β1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus. These results indicate that prenalterol possesses the ability to elicit a functional response by stimulation of either β1- or adrenoceptors provided that the tissue has a large spare receptor reserve for full agonists.
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| Type of Medium: |
Electronic Resource
|
| URL: |
| _version_ | 1798295840617398272 |
|---|---|
| autor | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. |
| autorsonst | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. |
| book_url | http://dx.doi.org/10.1007/BF00498518 |
| datenlieferant | nat_lic_papers |
| hauptsatz | hsatz_simple |
| identnr | NLM200611828 |
| issn | 1432-1912 |
| journal_name | Naunyn-Schmiedeberg's archives of pharmacology |
| materialart | 1 |
| notes | Summary Prenalterol, previously characterized as a functionally cardioselective partial β-adrenoceptor agonist, was shown to relax K+-elicited contractures in the uterine muscle from progesterone pretreated rats (pD 2 7.7) and to increase beating rate in the rat right atrium (pD 2 8.0) at about the same concentrations with maximal effects corresponding to 94 and 82% respectively of those of isoproterenol. Terbutaline, with equal maximal effects as isoproterenol, was 50 times more potent in the uterus (pD 2 7.8) than in the right atrium (pD 2 6.1). Both tissues displayed a high sensitivity to isoproterenol (pD 2 9.1 in both tisues) indicating large receptor reserves for the full agonist. The maximal relaxing effect of prenalterol in the uterus was obtained at about a three-fold increase of the cyclic AMP content, which is similar to that obtained with isoproterenol at a corresponding relaxation. The effects in the uterine muscle of all three agonists were mediated through β2-adrenoceptors since β2-adrenoceptor blockers (ICI 118,551 and IPS 339) antagonized the effects in concentrations which had only marginal effects on the atrial responses of the agonists. The β1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus. These results indicate that prenalterol possesses the ability to elicit a functional response by stimulation of either β1- or adrenoceptors provided that the tissue has a large spare receptor reserve for full agonists. |
| package_name | Springer |
| publikationsjahr_anzeige | 1982 |
| publikationsjahr_facette | 1982 |
| publikationsjahr_intervall | 8019:1980-1984 |
| publikationsjahr_sort | 1982 |
| publisher | Springer |
| reference | 321 (1982), S. 302-308 |
| schlagwort | Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP |
| search_space | articles |
| shingle_author_1 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. |
| shingle_author_2 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. |
| shingle_author_3 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. |
| shingle_author_4 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. |
| shingle_catch_all_1 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. β1 and β2 Stimulatory effects of prenalterol Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Summary Prenalterol, previously characterized as a functionally cardioselective partial β-adrenoceptor agonist, was shown to relax K+-elicited contractures in the uterine muscle from progesterone pretreated rats (pD 2 7.7) and to increase beating rate in the rat right atrium (pD 2 8.0) at about the same concentrations with maximal effects corresponding to 94 and 82% respectively of those of isoproterenol. Terbutaline, with equal maximal effects as isoproterenol, was 50 times more potent in the uterus (pD 2 7.8) than in the right atrium (pD 2 6.1). Both tissues displayed a high sensitivity to isoproterenol (pD 2 9.1 in both tisues) indicating large receptor reserves for the full agonist. The maximal relaxing effect of prenalterol in the uterus was obtained at about a three-fold increase of the cyclic AMP content, which is similar to that obtained with isoproterenol at a corresponding relaxation. The effects in the uterine muscle of all three agonists were mediated through β2-adrenoceptors since β2-adrenoceptor blockers (ICI 118,551 and IPS 339) antagonized the effects in concentrations which had only marginal effects on the atrial responses of the agonists. The β1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus. These results indicate that prenalterol possesses the ability to elicit a functional response by stimulation of either β1- or adrenoceptors provided that the tissue has a large spare receptor reserve for full agonists. 1432-1912 14321912 Springer |
| shingle_catch_all_2 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. β1 and β2 Stimulatory effects of prenalterol Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Summary Prenalterol, previously characterized as a functionally cardioselective partial β-adrenoceptor agonist, was shown to relax K+-elicited contractures in the uterine muscle from progesterone pretreated rats (pD 2 7.7) and to increase beating rate in the rat right atrium (pD 2 8.0) at about the same concentrations with maximal effects corresponding to 94 and 82% respectively of those of isoproterenol. Terbutaline, with equal maximal effects as isoproterenol, was 50 times more potent in the uterus (pD 2 7.8) than in the right atrium (pD 2 6.1). Both tissues displayed a high sensitivity to isoproterenol (pD 2 9.1 in both tisues) indicating large receptor reserves for the full agonist. The maximal relaxing effect of prenalterol in the uterus was obtained at about a three-fold increase of the cyclic AMP content, which is similar to that obtained with isoproterenol at a corresponding relaxation. The effects in the uterine muscle of all three agonists were mediated through β2-adrenoceptors since β2-adrenoceptor blockers (ICI 118,551 and IPS 339) antagonized the effects in concentrations which had only marginal effects on the atrial responses of the agonists. The β1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus. These results indicate that prenalterol possesses the ability to elicit a functional response by stimulation of either β1- or adrenoceptors provided that the tissue has a large spare receptor reserve for full agonists. 1432-1912 14321912 Springer |
| shingle_catch_all_3 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. β1 and β2 Stimulatory effects of prenalterol Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Summary Prenalterol, previously characterized as a functionally cardioselective partial β-adrenoceptor agonist, was shown to relax K+-elicited contractures in the uterine muscle from progesterone pretreated rats (pD 2 7.7) and to increase beating rate in the rat right atrium (pD 2 8.0) at about the same concentrations with maximal effects corresponding to 94 and 82% respectively of those of isoproterenol. Terbutaline, with equal maximal effects as isoproterenol, was 50 times more potent in the uterus (pD 2 7.8) than in the right atrium (pD 2 6.1). Both tissues displayed a high sensitivity to isoproterenol (pD 2 9.1 in both tisues) indicating large receptor reserves for the full agonist. The maximal relaxing effect of prenalterol in the uterus was obtained at about a three-fold increase of the cyclic AMP content, which is similar to that obtained with isoproterenol at a corresponding relaxation. The effects in the uterine muscle of all three agonists were mediated through β2-adrenoceptors since β2-adrenoceptor blockers (ICI 118,551 and IPS 339) antagonized the effects in concentrations which had only marginal effects on the atrial responses of the agonists. The β1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus. These results indicate that prenalterol possesses the ability to elicit a functional response by stimulation of either β1- or adrenoceptors provided that the tissue has a large spare receptor reserve for full agonists. 1432-1912 14321912 Springer |
| shingle_catch_all_4 | Mattsson, H. Andersson, T. Carlsson, E. Hedberg, A. Lundgren, B. Olsson, T. β1 and β2 Stimulatory effects of prenalterol Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Prenalterol Agonistic acitivity β-Adrenoceptors Spare receptors Cyclic AMP Summary Prenalterol, previously characterized as a functionally cardioselective partial β-adrenoceptor agonist, was shown to relax K+-elicited contractures in the uterine muscle from progesterone pretreated rats (pD 2 7.7) and to increase beating rate in the rat right atrium (pD 2 8.0) at about the same concentrations with maximal effects corresponding to 94 and 82% respectively of those of isoproterenol. Terbutaline, with equal maximal effects as isoproterenol, was 50 times more potent in the uterus (pD 2 7.8) than in the right atrium (pD 2 6.1). Both tissues displayed a high sensitivity to isoproterenol (pD 2 9.1 in both tisues) indicating large receptor reserves for the full agonist. The maximal relaxing effect of prenalterol in the uterus was obtained at about a three-fold increase of the cyclic AMP content, which is similar to that obtained with isoproterenol at a corresponding relaxation. The effects in the uterine muscle of all three agonists were mediated through β2-adrenoceptors since β2-adrenoceptor blockers (ICI 118,551 and IPS 339) antagonized the effects in concentrations which had only marginal effects on the atrial responses of the agonists. The β1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus. These results indicate that prenalterol possesses the ability to elicit a functional response by stimulation of either β1- or adrenoceptors provided that the tissue has a large spare receptor reserve for full agonists. 1432-1912 14321912 Springer |
| shingle_title_1 | β1 and β2 Stimulatory effects of prenalterol |
| shingle_title_2 | β1 and β2 Stimulatory effects of prenalterol |
| shingle_title_3 | β1 and β2 Stimulatory effects of prenalterol |
| shingle_title_4 | β1 and β2 Stimulatory effects of prenalterol |
| sigel_instance_filter | dkfz geomar wilbert ipn albert fhp |
| source_archive | Springer Online Journal Archives 1860-2000 |
| timestamp | 2024-05-06T09:42:36.338Z |
| titel | β1 and β2 Stimulatory effects of prenalterol |
| titel_suche | β1 and β2 Stimulatory effects of prenalterol |
| topic | WW-YZ |
| uid | nat_lic_papers_NLM200611828 |