Adrenergic Receptor Agonist

Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

Guanabenz (Acetate) (BR-750) is an alpha-2 selective adrenergic agonist used as an antihypertensive agent.

Fenoterol (Th-1165), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.

Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD).

Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion.

Terbutaline sulfate is an orally active β₂-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline sulfate can be used in asthma symptom research.

Synephrine (Oxedrine), an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine is a sympathomimetic compound and can be used for weight loss.

Guanabenz is an orally active α-2-adrenoceptor agonist. Guanabenz has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure.

Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma.

Xamoterol (Corwin; ICI 118587) hemifumarate is an orally active and selective β₁-adrenoceptor partial agonist. Xamoterol hemifumarate acts as agonist at low sympathetic tone, antagonist at high sympathetic tone, with context-dependent cardiovascular effects including modulated heart rate, blood pressure, and cardiac output. Xamoterol hemifumarate can be used for the research of heart failure, postural hypotension, and ischemic heart disease.

Vilanterol (GW642444) is a long-acting β₂ adrenergic receptor agonist. Vilanterol has pEC₅₀ values for β₂-AR, β₁-AR, and β₃-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol selectively activates airway β₂ adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol can be used in asthma research^[3][5].

A-61603 is a selective α₁A/α₁a-adrenergic receptor agonist with K_i of 8.89 nM for rat submaxillary gland α1A, K_i of 30.5 nM for cloned bovine α1a. A-61603 potentiates Ca²⁺ transients with EC₅₀ of 6.9 nM. A-61603 stimulates phosphoinositide hydrolysis, induces contractile responses in vas deferens, prostate strips, and spleen strips, and exhibits low activity in aortic rings. A-61603 can be used for research on adrenergic function.

Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC₅₀ of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.

Adrafinil (CRL 40028) is an orally active vigilance promoting agent. Adrafinil enhances central noradrenergic transmission, improves spontaneous activity, exploratory behavior, discriminative learning ability and response motivation, but impairs visuospatial working memory. Adrafinil antagonizes Prazosin (HY-B0193)-induced hypoactivity and hypothermia, exerts anticonvulsant effects, and induces sustained enhancement of high-frequency electrocortical activity. Adrafinil can be used for research on decreased alertness and specific cognitive deficits.

Olodaterol (BI1744) hydrochloride is a selective, long acting β₂-adrenoceptor (β₂-AR) agonist (EC₅₀=0.1 nM and pK_i= 9.14 for human β₂-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.

LY 344864 is a selective, orally active 5-HT_1F receptor agonist with a K_i of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.

Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research.

Medetomidine is an orally active α2-adrenoceptor agonist (K_i: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.

Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism.

Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.