Adrenergic Receptor Ligand

Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.

(+)-Niguldipine hydrochloride is a 1,4-DHP receptor ligand associated with L-type Ca²⁺ channels (with K_i values of 85 pmol/L in guinea pig skeletal muscle, 140 pmol/L in brain, and 45 pmol/L in heart) as well as an α₁-adrenergic receptor ligand (with a K_i value of 78 nmol/L). (+)-Niguldipine hydrochloride shows much higher binding selectivity for α_1α-adrenergic receptors than for α_1B-adrenergic receptors. (+)-Niguldipine hydrochloride can be used in studies related to hypertension.

Flavoxate (Rec-7-0040 free base; DW61 free base) is an orally active L-type Ca²⁺ channel inhibitor and antispasmodic. Flavoxate inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate can be used in research on overactive bladder and related voiding dysfunctions.

Iloperidone carboxylic acid (P95-12113) is the metabolite of Iloperidone (HY-17410). Iloperidone carboxylic acid exhibits good affinity for 5-HT2A receptor with pK_i of 8.15, and moderate affinity for adrenergic receptor α1/α2B/α2C.

Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.

Isamoltan ((±)-Isamoltane) hydrochloride is a selective antagonist of 5-HT_1B receptor, with an IC₅₀ of 39 nM for inhibits the binding of [¹²⁵I]ICYP to 5-HT_1B recognition sites in rat brain membranes. Isamoltan hydrochloride is also a β-adrenoceptor ligand, with an IC₅₀ of 8.4 nM. Isamoltan hydrochloride shows anxiolytic activity.

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

Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (K_i=198 nM), α2A adrenergic receptor (K_i=180 nM; EC₅₀=440 nM) and 5-HT_2A receptor (EC₅₀=172 nM, E_max=76%). Z8779877149 inhibits 5-HT reuptake and activates G_i and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.

Flavoxate-d₅ is deuterium labeled Flavoxate. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.

α1A-AR ligand-1 (Compound 3) is an α1A-AR ligand that can be used to synthesize PROTACs, such as α1A-AR Degrader 9c (HY-147100).

Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis.

3-MPPI is a GPCR ligand with high selectivity for α₁-adrenergic receptor, with a K_i value of 0.21 nM for α₁-adrenergic receptor and 50 nM for 5-HT₁A receptor. 3-MPPI modulates the α₁-adrenergic receptor signaling cascade. 3-MPPI is applicable to research related to hypertension, stress-induced anxiety-like behavioral responses, and levodopa-induced dyskinesia.

Metrazoline (o-Methyl-tracizoline) is the ligand for adrenergic receptor (low affinity) and imidazoline I2 receptor.

TDIQ hydrochloride is an analog of Amphetamine with high affinity for α2-adrenergic receptor. TDIQ hydrochloride is a selective α2-adrenoceptor ligand with the K_i values of 75 nM, 95 nM, and 65 nM for α2A-, α2B-, and α2C-adrenergic receptors, respectively.

AR ligand-50 (Compound 4) is an adrenergic receptor ligand (pK_i: 7.14 for human α2-adrenergic receptor on CHO cells). AR Ligand-50 can be used in the research of neurological disorders.

Flavoxate-d₄ hydrochloride (Rec-7-0040-d₄) is the deuterium labeled Flavoxate hydrochloride. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.