Adrenergic Receptors

Cat. No.

A34140

CAS No.

1029802-21-8

Platelet aggregation-IN-3

Platelet aggregation-IN-3 is a ligand for H2 histamine receptors, α2-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound effectively inhibits platelet aggregation induced by ADP and collagen and modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 shows potential for applications in antiplatelet therapy for cardiovascular diseases and in the prevention of cancer-related thrombosis and tumor metastasis.

Cat. No.

A46038

CAS No.

475110-48-6

Iloperidone carboxylic acid

Synonyms: P95-12113

Iloperidone carboxylic acid is a ligand targeting the 5-HT2A receptor. This metabolite of Iloperidone demonstrates a strong affinity for the 5-HT2A receptor, with a pKi value of 8.15, while also showing moderate binding affinity to adrenergic receptors α1, α2B, and α2C. It serves as a valuable reagent for research exploring neuropharmacology and the modulation of serotonergic signaling in various biological contexts.

Cat. No.

A58383

CAS No.

3051498-44-0

β2AR ligand 1

β2AR ligand 1 is a homobivalent bitopic ligand that targets the β2 adrenergic receptor (β2AR) by binding to both the orthosteric binding site (OBS) and metastable binding sites (MBS). This compound exhibits specific affinity for β2AR, facilitating the study of receptor activation and signaling pathways. It is valuable in research applications focused on cardiovascular function, asthma, and other conditions where β2AR modulation is of interest.

Cat. No.

A58403

CAS No.

116049-78-6

SB-206606

SB-206606 is a selective beta 3-adrenergic receptor (β3-AR) ligand, exhibiting a significantly higher affinity for β3-AR, being 76 times more potent than for beta 1 and beta 2-adrenergic receptors. This compound serves as a valuable tool for studying β3-AR-mediated pathways and their implications in metabolic processes. Its specificity makes it essential for research into obesity, diabetes, and cardiovascular diseases.

Cat. No.

A58484

CAS No.

130905-04-3

Phendioxan

Phendioxan is a selective adrenergic receptor ligand with a high binding affinity for the α(1)-adrenaline receptor subtype. Its facilitated membrane diffusion enhances its efficacy at the α(1d)-AR, supporting its potential in cardiovascular and neuropharmacological research. Docking simulations have elucidated the significant roles of polar, electrostatic, hydrophobic, and shape interactions of its phenoxy terminal substituents in ligand-receptor binding dynamics.

Cat. No.

A58498

CAS No.

245744-10-9

RWJ52353

RWJ52353 is a selective ligand targeting the α2D adrenoceptor, with notable binding affinities for the α2A, α2B, and α1 receptors, exhibiting Ki values of 1.5, 254, 621, and 443 nM, respectively. This compound demonstrates significant analgesic activity, as evidenced by its efficacy in the mouse abdominal irritation test, where it has an ED50 of 15.1 mg/kg. RWJ52353 is valuable for studies investigating pain mechanisms and the role of α2 adrenoceptors in analgesia.

Cat. No.

A58669

CAS No.

133399-65-2

3-MPPI

3-MPPI is a selective G protein-coupled receptor (GPCR) ligand with a strong affinity for the α1-adrenergic receptor, exhibiting a Ki value of 0.21 nM, while its activity on the 5-HT1A receptor is significantly lower at 50 nM. This compound effectively modulates the signaling pathways associated with the α1-adrenergic receptor. Research applications of 3-MPPI include studies on hypertension, the effects of stress-induced anxiety-like behavior, and investigations into levodopa-induced dyskinesia.

Cat. No.

A58715

CAS No.

221225-04-3

Metrazoline

Synonyms: o-Methyl-tracizoline

Metrazoline is an imidazoline I2 receptor ligand with low affinity for adrenergic receptors. This compound is used in research to study its role in modulating neuroprotective and antihypertensive effects. It serves as a valuable tool for investigating the physiological and pharmacological functions associated with imidazoline receptors in both in vitro and in vivo settings.

Cat. No.

A58718

CAS No.

15052-05-8

TDIQ hydrochloride

TDIQ hydrochloride is a selective ligand for the α2-adrenergic receptors, exhibiting high affinity with Ki values of 75 nM, 95 nM, and 65 nM for the α2A, α2B, and α2C subtypes, respectively. This compound serves as a valuable tool for studying the physiological roles of α2-adrenoceptors and their potential therapeutic applications in various neuropsychiatric and cardiovascular disorders. Its specificity makes it suitable for pharmacological investigations and drug development in receptor-targeted therapies.

Cat. No.

A58763

CAS No.

158198-45-9

CHIR-2279

CHIR-2279 is a high-affinity ligand for the α1-adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 5 nM. This compound serves as a valuable tool for investigating the α1-adrenoceptor signaling pathways and has potential applications in drug development aimed at cardiovascular and other relevant disorders.

Cat. No.

A58806

CAS No.

501-62-2

AR ligand-50

AR Ligand-50 is an adrenergic receptor ligand with a pKi value of 7.14 for the human α2-adrenergic receptor, assessed in CHO cells. This compound demonstrates significant biological activity that can be utilized in the investigation of neurological disorders. Its potential therapeutic implications make it a valuable tool for research focused on adrenergic signaling pathways and related disease mechanisms.