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Dia-Prńsentation von Merck Gesellschaft mbH.
CIBIS II - Cardiac Insufficiency Bisoprolol Study (12 Abbildungen)
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Abb. 0: F▄R ÍSTERREICH: Weitere Informationen: Merck Gesellschaft mbH, Zimbagasse 5, 1147 Wien, Tel.: 01/576 00-0 Abb. 1: CIBIS II - Cardiac Insufficiency Bisoprolol Study Aktuelles Bild - Abb. 2: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Objectives Abb. 3: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Main inclusion criteria Abb. 4: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Design Abb. 5: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Characteristics (I) Abb. 6: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Characteristics (II) Zum letzten Bild
Abbildung 2: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Objectives
Bisoprolol proved to be the compound with the highest ▀1-selectivity in all in vitro and in vivo studies and in all animal species investigated. One measure of ▀1-selectivity is the ratio of the constants of inhibition (ci) for the ▀1- and ▀2-receptor. The constants of inhibition of the ▀-blockers bisoprolol, atenolol, betaxolol and propranolol were determined in ligand-binding studies using rat parotid gland (mainly occupied by ▀1-receptors) and rat reticulocytes (mainly occupied by ▀2-receptors) in human plasma: using a non-specific radiolabelled ligand, the ▀1- and ▀2-receptors of the rat parotid gland and reticulocytes were completely occupied. This cell suspension was then mixed with the plasma of volunteers pretreated with different ▀-blockers. The non-specific radioligand was now displaced from the receptor by addition of this serum enriched with ▀-blockers. Constants of inhibition of a characteristic magnitude for each ▀-blocker and receptor type could be determined from these tests; the smaller the ci-value, the higher the affinity of the ▀-blocker for the receptor type concerned. The ratio of ci/▀1 to ci/▀2 was 1:75 for bisoprolol, 1:35 for atenolol and betaxolol, 1:20 for metoprolol, and 1.8:1 for propranolol. Bisoprolol therefore proved to be the ▀-blocker with the highest ▀1-selectivity in this model as well.
 
CIBIS II - Cardiac Insufficiency Bisoprolol Study - Objectives
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Abbildung 2: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Objectives
Bisoprolol proved to be the compound with the highest ▀1-selectivity in all in vitro and in vivo studies and in all animal species investigated. One measure of ▀1-selectivity is the ratio of the constants of inhibition (ci) for the ▀1- and ▀2-receptor. The constants of inhibition of the ▀-blockers bisoprolol, atenolol, betaxolol and propranolol were determined in ligand-binding studies using rat parotid gland (mainly occupied by ▀1-receptors) and rat reticulocytes (mainly occupied by ▀2-receptors) in human plasma: using a non-specific radiolabelled ligand, the ▀1- and ▀2-receptors of the rat parotid gland and reticulocytes were completely occupied. This cell suspension was then mixed with the plasma of volunteers pretreated with different ▀-blockers. The non-specific radioligand was now displaced from the receptor by addition of this serum enriched with ▀-blockers. Constants of inhibition of a characteristic magnitude for each ▀-blocker and receptor type could be determined from these tests; the smaller the ci-value, the higher the affinity of the ▀-blocker for the receptor type concerned. The ratio of ci/▀1 to ci/▀2 was 1:75 for bisoprolol, 1:35 for atenolol and betaxolol, 1:20 for metoprolol, and 1.8:1 for propranolol. Bisoprolol therefore proved to be the ▀-blocker with the highest ▀1-selectivity in this model as well.
 
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