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.

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.

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.

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.

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