[On the pharmacology of the alpha-receptor blocker BE 2254 (HEAT) (author's transl)].
The alpha-adrenolytic activity of BE 2254 was investigated in in vitro as well as in vivo assays. On the isolated rat anococcygeus muscle, 2-[beta-(4-hydroxyphenyl)-ethyl-amino-methyl]tetralone(1) (BE 2254) shows a high affinity for postsynaptic alpha-adrenoceptors (pA2 = 8.9), in contrast to its much weaker potency (pA2 = 6.7) in inhibiting clonidine on the electrically driven rat vas deferens, thus suggesting a relative preference for postsynaptic alpha-adrenoceptors. BE 2254 effects on other catecholamine receptors are either negligible or not detectable. The hypotensive action of BE 2254 is shown to be solely due to alpha-blockade. All alpha-adrenolytic actions studied were of competitive nature.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D006168:Guinea Pigs; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009132:Muscles / Q000294:innervation; D009200:Myocardial Contraction / Q000187:drug effects; D009281:Naphthalenes / Q000494:pharmacology*; D009638:Norepinephrine / Q000494:pharmacology; D010627:Phenethylamines / Q000494:pharmacology*; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D012110:Reserpine / Q000494:pharmacology; D013569:Synapses / Q000187:drug effects; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D044024:Tetralones
D000317:Adrenergic alpha-Antagonists; D009281:Naphthalenes; D010627:Phenethylamines; D011942:Receptors, Adrenergic, alpha; D013764:Tetrahydronaphthalenes; D044024:Tetralones; C010652:BE 2254; D012110:Reserpine; D009638:Norepinephrine
Zur Pharmakologie des alpha-Rezeptoren-Blockers BE 2254 (HEAT).