Adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine and epinephrine. Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. The sympathetic nervous system is responsible for the fight-or-flight response, which includes widening the pupils of the eye, mobilizing energy, and diverting blood flow from non-essential organs to skeletal muscle. There are two main groups of adrenergic receptors, α and β, with several subtypes. α receptors have the subtypes α1 and α2. β receptors have the subtypes β1, β2 and β3. All three are linked to Gs proteins, which in turn are linked to adenylate cyclase. Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates some of the intracellular events following hormone binding.
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AGN192836 (AGN 192836) is a potent, selective α2 adrenergic (alpha 2-adrenoceptor) agonist with EC50 of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively; displays 1200-, 50- and 10-fols selectivity for the α2A-receptor, α2B-receptor, and α2C-receptors relative to the α2C-receptors; demonstrates effectivity for the reduction of intraocular pressure and for the reduction of blood pressure in vivo.
Olodaterol hydrochloride (BI1744 CL) is a potent, selective long-acting β2 adrenoceptor agonist with EC50 of 1.4 nM for hβ2; shows >250 fold selectivity over hβ1; exerts a bronchodilatory efficacy over 24 h in dogs and guinea pigs in the absence of systemic pharmacodynamic effects.
Dexmedetomidine hydrochloride is an agonist of α2-adrenergic receptor that used in veterinary medicine for its analgesic and sedative properties; also protects against lung injury induced by ischemia-reperfusion through inhibition of autophagy in rats.
TAK-259 hydrochloride (TAK259;TAK 259) is a potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM; displays 200-fold and 800-fold selectivity against α1A- and α1B-AR, respectively; shows antagonistic activity by a bladder strip test in rats with bladder outlet obstruction, ameliorates cystitis-induced urinary frequency in rats.
TAK-259 (TAK259;TAK 259) is a potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM; displays 200-fold and 800-fold selectivity against α1A- and α1B-AR, respectively; shows antagonistic activity by a bladder strip test in rats with bladder outlet obstruction, ameliorates cystitis-induced urinary frequency in rats.
MSX-3 hydrate is a potent, specific adenosine A2A receptor (A2AR) antagonist.
(S)-Timolol maleate is a potent non-selective β-adrenergic receptor antagonist with Ki of 1.97 and 2 nM for β1 and β2 receptor, respectively.
MK-4618 (MK 4618;MK4618;Vibegron;KRP-114V;RVT-901) is a potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM; displays no activity for β1 and β2 receptors (EC50>20 uM); dose-dependently increases bladder capacity, decreased micturition pressure, and increased bladder compliance in rhesus monkeys, dose-dependently increases the circulating glycerol and fatty acid levels in rhesus and rat in vivo; shows the potential for treatment of overactive bladder with M2/M3 antimuscarinics.
An α2 adrenergic receptor that is used as an antihypertensive drug; has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-PPP1R15A holophosphatase complex; also has antiparasitic activity against replicative stages of Toxoplasma.
Acebutolol is a cardioselective beta blocker for the treatment of hypertension and arrhythmias.
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