Bisoprolol, sold under the brand name Zebeta among others, is a beta blocker which is selective for the beta-1 receptor and used for cardiovascular diseases, including tachyarrhythmias, high blood pressure, angina, and heart failure. It is taken by mouth.
The alpha-2 (α2) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-, α2B-, and α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central and peripheral nervous systems.
Cirazoline is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α2 adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.
The alpha-1A adrenergic receptor, also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it. There is no longer a subtype α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, the naming convention was continued with the letter D.
The alpha-1D adrenergic receptor, also known as ADRA1D, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.
Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist. Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist, this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum. Unlike some other α1-adrenoceptor antagonists, urapidil does not elicit reflex tachycardia, and this may be related to its weak β1-adrenoceptor antagonist activity, as well as its effect on cardiac vagal drive. Urapidil is currently not approved by the U.S. Food and Drug Administration, but it is available in Europe.
Tretoquinol is a beta-adrenergic agonist.
Cyanopindolol is a drug related to pindolol which acts as both a β1 adrenoceptor antagonist and a 5-HT1A receptor antagonist. Its radiolabelled derivative iodocyanopindolol has been widely used in mapping the distribution of beta adrenoreceptors in the body.
SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies.
Dihydroalprenolol (DHA) is a hydrogenated alprenolol derivative that acts as a beta-adrenergic blocker. When the extra hydrogen atoms are tritium, it is a radiolabeled form of alprenolol, which is used to label beta-adrenergic receptors for isolation.
BRL-44408 is a drug used in scientific research which acts as a selective antagonist for the α2A adrenoreceptor. It has been suggested as having potential therapeutic application in the treatment of extrapyramidal side effects produced by some antipsychotic medications.
Corynanthine, also known as rauhimbine, is an alkaloid found in the Rauvolfia and Corynanthe genera of plants. It is one of the two diastereoisomers of yohimbine, the other being rauwolscine. It is also related to ajmalicine.
6-Fluoronorepinephrine (6-FNE) is a selective α1- and α2-adrenergic receptor full agonist related to norepinephrine. It is the only selective full agonist for the α-adrenergic receptors known to date and has been used to study their function in scientific research. Infusion of 6-FNE into the locus coeruleus of rodents produces marked hyperactivity and behavioral disinhibition by suppressing activity in the area via stimulation of α1-adrenergic receptors.
Fluparoxan is a potent α2-adrenergic receptor antagonist with excellent selectivity for this receptor over the α1-adrenergic receptor (2,630-fold), and is the only well-studied α2-adrenergic receptor antagonist in its structural family which does not antagonize any variant of the imidazoline receptor. It was shown to possess central α2-adrenoceptor antagonist activity after oral doses in man and was patented as an antidepressant by Glaxo in the early 1980s, but its development was discontinued when the compound failed to show a clear clinical advantage over existing therapies.
Domesticine is an α1D-adrenergic receptor antagonist. The compound belongs to the group of Aporphine alkaloids.
Zolertine is an alpha-1 adrenoceptor antagonist.
Bufetolol is a beta-adrenoceptor antagonist.
Exaprolol is a beta-adrenoceptor antagonist.
Nifenalol is a beta-adrenoceptor antagonist.
Eugenodilol is an alpha-1 blocker and beta blocker with weak β2-adrenergic receptor agonist activity derived from eugenol.
