Adrenergic Receptor Modulator

DL-Norepinephrine-d₆ hydrochloride is the deuterium labeled DL-Norepinephrine hydrochloride. DL-Norepinephrine hydrochloride is an external racemic catecholamine neurotransmitter, which is an equal mixture of the left-handed (L-, with activity) and right-handed (D-, with very low or no activity) stereoisomers. DL-Norepinephrine hydrochloride after being labeled with tritium can be used as a tracer for the research on Parkinson's disease.

DL-Norepinephrine hydrochloride is an external racemic catecholamine neurotransmitter, which is an equal mixture of the left-handed (L-, with activity) and right-handed (D-, with very low or no activity) stereoisomers. DL-Norepinephrine hydrochloride after being labeled with tritium can be used as a tracer for the research on Parkinson's disease.

Lubabegron is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron demonstrates antagonistic behavior at the β₁ and β ₂ receptor subtypes and agonistic behavior at the β ₃ receptor subtype in cattle. Lubabegron reduces NH₃ gas emissions from an animal or its waste. Lubabegron is available as an animal supplement.

DL-Norepinephrine tartrate is an external racemic catecholamine neurotransmitter, which is an equal mixture of the left-handed (L-, with activity) and right-handed (D-, with very low or no activity) stereoisomers. DL-Norepinephrine tartrate after being labeled with tritium can be used as a tracer for the research on Parkinson's disease.

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

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

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.

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β₃-AR (K_i = 88 nM) agonist with β₁/β₂-AR (K_i = 0.9 nM for β₁; K_i = 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.

NRA‑0562 is a dopamine antagonist with high affinities for dopamine D₁/D₂/D₃/D₄, 5‑HT₂A and α₁‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED₅₀ = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..

GLPG0492-¹³C,d₃ racemate is ¹³C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy.

Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of ³H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist.

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

ABT-866 is an α_1A-adrenoceptor agonist and an antagonist at the α_1B- and α_1D-adrenoceptor subtypes. ABT-866 has an EC₅₀ of 0.60 μM for the α_1A in the rabbit urethra. ABT-866 has a pA₂ value of 5.4 for the α_1B in the rat spleen. ABT-866 has a pA₂ value of 6.2 for the α_1D 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.

Vasorelaxant agent-2 (Compound 8h) targets α1A-adrenergic receptor with an affinity of pD2=5.4. Vasorelaxant agent-2 exhibits vasodilator activity in rats aortic rings with an EC₅₀ of 0.79 μM.

α1 adrenoceptor-MO-1, an S enantiomer, has affinity at alpha 1 adrenergic receptor, shows alphalytic activity, and possesses analgesic action; more active than R enantiomer.

D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.