α2c adrenergic receptor

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

JP1302 is a selective α2C adrenoceptor antagonist with a Kb value of 16 nM and a Ki of 28 nM for human α2C receptors.JP1302 has antidepressant activity, disrupts the FACT complex and degrades histone H1.JP1302 has been used in the study of neuropsychiatric disorders, acute renal failure, and renal injury.

Xylometazoline hydrochloride (Xylometazoline HCl) is an α-adrenoceptor agonist usually used as nasal decongestant.

Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.

Guanabenz Acetate (Wytensin) is a specific agonist of adrenergic receptor. The pEC50 for α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor is 8.25, 7.01 and ~5, respectively.

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7 nM, 41 nM, and 6.6 nM for the α2A, α2B, and α2C receptors, respectively.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

Benzquinamide (P2647), an antiemetic agent with anticancer activity, inhibits p-glycoprotein-mediated drug efflux and potentiates the cytotoxicity of anticancer drugs in multidrug-resistant cells.The Ki values of Benzquinamide for α2A, α2B, and α2C adrenergic receptor (α2-AR) were 1,365, 691, and 545 nM, respectively. 545 nM, respectively.

OPC-28326 is a specific an α2-adrenergic receptor antagonist and acts as a peripheral vasodilator. OPC-28326 inhibits α2A-, α2B- and α2C-adrenoceptors with Ki of 2040, 285, and 55 nM, respectively.

ORM-10921 is an α2C-adrenoceptor antagonist that has shown antipsychotic and antidepressant activity in animal studies.

Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.

JP1302 dihydrochloride is a selective, high affinity antagonist of the alpha2C-adrenoceptor (α2C-adrenoceptor), with a Ki (binding affinity) value of 28 nM and a Kb value (antagonist activity) of 16 nM.

(S)-Terazosin is an active S-enantiomer of Terazosin and acts as a potent, high-affinity antagonist of α-adrenoceptors [α1a, α1b, and α1d-adrenoceptors] with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, respectively.

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

The pKi values of Allyphenyline oxalate (compound 9) for the α2-adrenergic receptor subtypes α2A, α2B, and α2C are 7.24, 6.47, and 7.07, respectively.

Benalfocin hydrochloride is a potent and selective α2-adrenergic receptor antagonist that blocks α2A, α2B, and α2C receptor subtypes with high affinity, Benalfocin hydrochloride is widely employed in neuroscience research to dissect adrenergic signaling pathways by inhibiting adrenaline-mediated effects on neurotransmission, autonomic regulation, and central nervous system function.

BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.

Guanfacine-13C,15N3 is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine (T22824) is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).

Iloperidone metabolite P95 is a metabolite of the atypical antipsychotic iloperidone . It binds to the serotonin (5-HT) receptor subtype 5-HT2A and α1-, α2B-, and α2C-adrenergic receptors with mean Ki values of 7.08, 21.38, 83.18, and 47.86 nM, respectively, but does not cross the blood-brain barrier.

Lurasidone-D8 hydrochloride is a deuterated compound of Lurasidone hydrochloride. Lurasidone hydrochloride has a CAS number of 367514-88-3. Lurasidone hydrochloride (T1735) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.