An α2-AR agonist (Kis = 61.66

Clonidine (hydrochloride) – 500 mg

Brand:
Cayman
CAS:
4205-91-8
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Clonidine is an agonist of α2-adrenergic receptors (α2-ARs; Kis = 61.66, 69.18, and 134.9 nM for α2A-, α2B-, and α2C-ARs, respectively).{40326} It stimulates [35S]GTPγS binding to HEK293 cell membranes expressing the human receptors with EC50 values of 26.92, 56.23, and 912.01 nM for α2A-, α2B-, and α2C-ARs, respectively. Clonidine also binds to I1-imidazoline sites in a variety of cell and tissue types (Kds = 4-15 nM).{46373} It induces relaxation of isolated mesenteric artery rings precontracted with norepinephrine (Item No. 16673) when used at a concentration of 10 μM.{25849} Clonidine (10 μM) also induces membrane hyperpolarization and reduces norepinephrine-induced depolarization in isolated mesenteric artery rings. Clonidine (0.1 and 1 μg/kg) reduces mean blood pressure and heart rate when administered via microinjection to the nucleus reticularis lateralis (NRL) of anesthetized normotensive cats.{36359} Formulations containing clonidine have been used in the treatment of hypertension.  

 

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Description

An α2-AR agonist (Kis = 61.66, 69.18, and 134.9 nM for α2A-, α2B-, and α2C-ARs, respectively); stimulates [35S]GTPγS binding to HEK293 cell membranes expressing human receptors (EC50s = 26.92, 56.23, and 912.01 nM for α2A-, α2B-, and α2C-ARs, respectively); binds to I1-imidazoline sites in a variety of cell and tissue types (Kds = 4-15 nM); induces relaxation of isolated mesenteric artery rings precontracted with norepinephrine at 10 μM; induces membrane hyperpolarization and reduces norepinephrine-induced depolarization in isolated mesenteric artery rings at 10 μM; reduces mean blood pressure and heart rate when administered via microinjection to the NRL of anesthetized normotensive cats at 0.1 and 1 μg/kg

Formal name: N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine, monohydrochloride

Synonyms:  ST 155

Molecular weight: 266.6

CAS: 4205-91-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Neuroscience

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