Studies on the receptor profile of bisoprolol.
The in vitro binding affinity of (+/-)-1-[4-(2-isopropoxyethoxymethyl)-phenoxy]-3-isopropylamino-2- propranol hemifumarate (bisoprolol, EMD 33 512) to beta 1-, beta 2-, alpha 1-, alpha 2-, D1-, D2-, 5-HT2- and muscarinic cholinergic receptors of rat was compared with that of atenolol, betaxolol and propranolol. Bisoprolol showed a high specific binding affinity to beta 1-adrenoceptors (heart) and a low specific binding affinity to beta 2-adrenoceptors (lung). The beta 1-selectivity of bisoprolol (beta 2/beta 1 = 34.7) proved to be higher than that of atenolol (8.7) and betaxolol (12.5). Propranolol (0.59) was non-selective as expected. Bisoprolol and atenolol exhibited no remarkable binding affinity to alpha 1-, alpha 2-, D1-, D2-, 5-HT2- and muscarinic cholinergic receptors at concentrations up to 1 X 10(-4) mol/l. For betaxolol binding affinities for alpha 2-, D2- and 5-HT2-receptors were found with IC50 values ranging between 2 X 10(-5) and 7 X 10(-5) mol/l. For propranolol binding affinities for alpha 1-, alpha 2-, D1-, D2- and 5-HT2-receptors were found with IC50 values ranging between 2 X 10(-6) and 9 X 10(-5) mol/l.
Klockow
M
M
Greiner
H E
HE
Haase
A
A
Schmitges
C J
CJ
Seyfried
C
C
D000319:Adrenergic beta-Antagonists / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D017298:Bisoprolol; D002417:Cattle; D004082:Dihydroalprenolol; D004294:Domperidone / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007650:Ketanserin; D008297:Male; D010880:Piperidines / Q000378:metabolism; D011224:Prazosin / Q000378:metabolism; D011412:Propanolamines / Q000378:metabolism* / Q000494:pharmacology; D011813:Quinuclidinyl Benzilate; D051381:Rats; D011919:Rats, Inbred Strains; D011941:Receptors, Adrenergic / Q000187:drug effects / Q000378:metabolism*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism*; D011968:Receptors, Histamine / Q000378:metabolism*; D011976:Receptors, Muscarinic / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism; D013764:Tetrahydronaphthalenes; D015016:Yohimbine / Q000378:metabolism
D000319:Adrenergic beta-Antagonists; D010880:Piperidines; D011412:Propanolamines; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; D011954:Receptors, Dopamine; D011968:Receptors, Histamine; D011976:Receptors, Muscarinic; D013764:Tetrahydronaphthalenes; D015016:Yohimbine; D013134:Spiperone; C011639:ADTN; D004294:Domperidone; D004082:Dihydroalprenolol; D011813:Quinuclidinyl Benzilate; D007650:Ketanserin; D011224:Prazosin; D017298:Bisoprolol