Partial agonistic activity of two irreversible beta-adrenergic receptor ligands, bromoacetylated derivatives of alprenolol and pindolol.
Our data demonstrate that the irreversible beta-adrenergic receptor probes BAAM and BIM are partial agonists. They should be used with caution until the impact of this finding on estimates of agonist affinity, non-linear receptor-effector coupling and receptor metabolism can be more precisely defined.
Jasper
J R
JR
Department of Pharmacology, University of California, San Diego, La Jolla 92093.
Michel
M C
MC
Insel
P A
PA
D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000526:Alprenolol / Q000031:analogs & derivatives* / Q000494:pharmacology; D002460:Cell Line / Q000187:drug effects / Q000378:metabolism; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D000081005:Cyclohexane Monoterpenes; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010869:Pindolol / Q000031:analogs & derivatives* / Q000494:pharmacology
D000318:Adrenergic beta-Agonists; D000081005:Cyclohexane Monoterpenes; C057316:N(8)-bromoacetyl-N(1)-3'-(4-indolyloxy)-2'-hydroxypropyl-1,8-diamino-4-menthane; D005576:Colforsin; C045331:bromoacetylalprenololmenthane; D000526:Alprenolol; D010869:Pindolol; D000242:Cyclic AMP