title: Interactions of carteolol and other beta-adrenoceptor blocking agents with serotonin receptor subtypes.
abstract: The importance of the anti-serotonergic activity of carteolol and other beta-adrenoceptor blockers in their efficacy as anti-migraine agents has been examined in the membrane fraction of rat brain frontal cortex and pig choroid plexus, using radioligand binding methods. Carteolol and l-propranolol, which are suggested to have anti-migraine activity in man, were found to be active inhibitors of the binding of [125I]ICYP to 5-HT1B recognition sites and of [3H]-8-OH-DPAT to 5-HT1A recognition sites. Carteolol is devoid of activity at 5-HT1C and 5-HT2 recognition sites, whereas l-propranolol shows substantial affinity for these receptor subtypes. Atenolol, another beta-adrenoceptor blocker with anti-migraine activity, is devoid of activity at any of the 5-HT receptor subtypes examined. The possibility that carteolol and other beta-adrenoceptor antagonists exert their pharmacological effects through central 5-HT receptor subtypes is discussed in relation to the potential mechanism of the anti-migraine activity of carteolol.
authors.affiliation: Department of Pharmacology, Hiroshima University School of Medicine, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Nishio
authors.forename: Y
authors.initials: Y
authors.lastname: Nagakura
authors.forename: T
authors.initials: T
authors.lastname: Segawa
mesh_terms: D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000319:Adrenergic beta-Antagonists / Q000378:metabolism*; D000818:Animals; D002354:Carteolol / Q000378:metabolism*; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D002831:Choroid Plexus / Q000187:drug effects / Q000378:metabolism; D004873:Ergolines / Q000378:metabolism; D066298:In Vitro Techniques; D020120:Iodocyanopindolol; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D010869:Pindolol / Q000031:analogs & derivatives; D011412:Propanolamines / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000378:metabolism*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology
chemical_list: D000319:Adrenergic beta-Antagonists; D004873:Ergolines; D011412:Propanolamines; D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D020120:Iodocyanopindolol; D002354:Carteolol; D010869:Pindolol; C031649:mesulergine