XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research.

Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

LM-189, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 can be used to develop the Gαi-biased β2AR agonists.

LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists.

VUF26034 (Compound 12b) is a photoresponsive ligand for the human β2-adrenergic receptor (β2-AR.

ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence.

L742791 is a β3-AR agonist. L742791 elicits lipolytic response in isolated nonhuman primate adipocytes.

GG-818 is a potent and selective α1 adrenoceptor antagonist, with pKi values of 9.7 for α1a, 7.8 for α1b, and 7.6 for α1d. GG-818 can be used for benign prostatic hyperplasia research.

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity.

L-657743 is a highly potent, highly selective, and orally active α2-adrenoceptor antagonist. L-657743 can be used in the research of neurological diseases such as depression.

CP-114271 is a potent selective β3-adrenergic receptor agonist. CP-114271 possesses an in vivo efficacy in rodent models. CP-114271 can be used for obesity research.

CP-331684 is an orally active agonist of β3-Adrenergic receptor. CP-331684 can be studied in research on obesity.

BRL-26830A is a β-adrenergic receptor agonist. In obese mouse models, BRL-26830A reduces body weight and increases metabolic rate. BRL-26830A stimulates insulin release and significantly reduces blood glucose levels in ICR mouse models. BRL-26830A can be used to study endocrine and metabolic diseases such as obesity and diabetes.

SGB-1534 (hydrochloride) is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 (hydrochloride) can inhibit vasoconstriction and lower blood pressure. SGB-1534 (hydrochloride) can be used for the research of cardiovascular disease, such as hypertension.

Carbuterol (SKF 40383-A) is a selective β2-adrenergic receptor agonist that primarily targets bronchial smooth muscle, exhibiting significant bronchodilatory and anti-allergic activity. Carbuterol can directly inhibit the immunologically induced release of histamine and slow-reacting substance of anaphylaxis (SRS-A), thereby alleviating allergic responses. Carbuterol exerts mild β1-mediated cardiac stimulation and is applicable to studies related to respiratory and immune-related diseases such as asthma and allergic disorders.

LY377604 hydrochloride is a human β3-adrenergic receptor agonist with an EC50 of 2.4 nM and also a β1- and β2-adrenergic receptor antagonist.

GYKI 12743 is a vasoselective, postsynaptic α-adrenoceptor blocker. GYKI 12743 inhibits but does not completely eliminate the cutaneous microcirculatory blood flow reduction evoked by electrical stimulation of the peripheral stump of the cut saphenous nerve in rats. GYKI 12743 can be used for the study of neurological diseases.

Butopamine is the active R/R stereoisomer butapamine of ractopamine hydrochloride. Butopamine exerts its physiological effects by stimulating β1-adrenergic receptor (β1AR) and β2-adrenergic receptor (β2AR) expressed in skeletal muscle and adipose tissue.

Nebivolol O-β-D-glucuronide is a derivative of Nebivolol. Nebivolol is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.

DL-017 is a Quinazoline derivative. DL-017 shows inhibitory constants of approximately 0.90 nM for α1-adrenergic receptors and 404 nM for Na+ channels. DL-017 exerts antihypertensive effect.

BMS-210285 is a highly selective agonist for the β3 receptor. BMS-210285 can be studied for obesity and type 2 diabetes research.

IP-66 is a potent postsynaptic alpha-receptor antagonist. IP-66 can be used for the research of cardiovascular disease, such as hypertension.

β-Blocker B-24/76 is a beta adrenoceptor blocker. β-Blocker B-24/76 exhibits beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties. β-Blocker B-24/76 can suppress the increased ornithine decarboxylase activity in hypertrophied hearts. β-Blocker B-24/76 can be used for the research of cardiovascular disease.

(±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH.

BRL 35135 is a potent and selective β3-adrenergic receptor agonist. BRL 35135 can dose dependently increase energy expenditure, reduce weight, and only reduce fat without reducing muscle protein. BRL 35135 can significantly improve glucose tolerance and insulin sensitivity. BRL 35135 can be used to study metabolic conditions such as obesity and diabetes.

BRL-41992 is a selective α₂B-adrenergic receptor antagonist. BRL-41992 exhibits 94-fold higher selectivity for the α₂B-receptor than for the α₂A-receptor with Kᵢ values in neonatal rat lung tissue (expressing the α₂B-receptor) and in human platelet membranes (expressing the α₂A-receptor) of 1.1 and 103.3 nM. BRL-41992 can be used to verify the functional differences of α₂ receptor subtypes.

RS-79948-197 hemihydrate is a non-imidazoline α2-adrenoceptor antagonist. RS-79948-197 hemihydrate shows Kd values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively.

MEPB is a modulator of AF-2 of the androgen receptor. MEPB increases co-repressor binding of AR. MEPB can bind to the BF3 pockeet of AR specifically, thereby modulating the binding of co-regulators to the AF2 domain. MEPB alleviates degeneration in spinal bulbar muscular atrophy mouse model.

4-Hydroxy xylazine O-glucuronide (lithium) is a metabolite of the α2-adrenergic receptor agonist xylazine. 4-Hydroxy xylazine O-glucuronide (lithium) can be synthesized from xylazine via the intermediate metabolite 4-hydroxy xylazine.