[Pharmacological characteristics of the long-acting beta-blocker "bopindolol"].
The non-selective beta-blocker bopindolol, which was developed as a pro-drug, possessed 50-60 times more potent long-acting hypotensive effects on the blood pressure than those of atenolol or propranolol. Because this drug has only a mild partial agonist activity, it did not cause the rapid decrease in heart rate observed with atenolol or propranolol or the increase in heart rate induced by pindolol. These hypotensive effects are due to beta 1-antagonistic effects, not effects on beta 2- or beta 3-adrenoceptors. In addition to these effects, benefits of this drug include the following: slow dissociation rate from beta-adrenoceptors in tissues, high affinity to 5-HT1A subtypes, less clinical effects on lipid metabolism and the inhibition of renin release. It is possible that this drug possesses different pharmacological characteristics from other beta-blockers.
Nagatomo
T
T
Department of Pharmacology, Niigata College of Pharmacy, Japan.
Hosohata
Y
Y
Ohnuki
T
T
Suzuki
J
J
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology; D002462:Cell Membrane / Q000187:drug effects; D006321:Heart / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D010869:Pindolol / Q000031:analogs & derivatives* / Q000494:pharmacology; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects; D012083:Renin / Q000378:metabolism; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D018340:Receptors, Adrenergic, alpha-1; D011985:Receptors, Serotonin; D010869:Pindolol; D012083:Renin; C036007:bopindolol