• In contrast, clonidine binds to both receptors with near equal affinity. (wikipedia.org)
  • Also, guanidinium derivatives show the ability to activate imidazoline receptors. (hindawi.com)
  • Meanwhile, only agmatine-induced relaxation was abolished by BU224, a selective antagonist of imidazoline I 2 -receptors. (hindawi.com)
  • Imidazoline receptors are introduced to play a role in cardiovascular regulation [ 2 , 3 ]. (hindawi.com)
  • The clinical used antihypertensive agent rilmenidine may reduce blood pressure via an activation of imidazoline I 1 -receptors in brain to lower sympathetic tone [ 8 , 9 ]. (hindawi.com)
  • It has been documented that compounds with guanidine-like structures may bind to imidazoline receptors [ 11 ]. (hindawi.com)
  • Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). (wikipedia.org)
  • In addition, moxonidine may also promote sodium excretion, improve insulin resistance and glucose tolerance and protect against hypertensive target organ damage, such as kidney disease and cardiac hypertrophy. (wikipedia.org)
  • Environmental factors such as a stressful lifestyle, a high sodium intake in the diet, obesity, and smoking all contribute to the development of hypertension. (alldaytrending.com)
  • Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of mild to moderate essential hypertension. (wikipedia.org)
  • Hypertension, often known as high blood pressure, is a highly common and serious illness that may lead to or worsen a variety of health problems Hypertension is a chronic medical disorder characterized by excessive blood pressure in the arteries. (alldaytrending.com)
  • It has been indicated that activation of peripheral imidazoline I 2 -receptor (I-2R) may reduce the blood pressure in spontaneously hypertensive rats (SHRs). (hindawi.com)
  • Effects on insulin resistance In all animal models of insulin resistance, moxonidine had striking effects on the development of insulin resistance, hyperinsulinaemia and impaired glucose homeostasis. (wikipedia.org)
  • If concomitant treatment with a beta blocker has to be stopped, the beta blocker should be discontinued first, then moxonidine after a few days. (wikipedia.org)
  • In this study, a series of doses of four imidazoline and two nonimidazoline antihypertensive drugs were administered by intracisternal (i.c.) injection to freely moving spontaneously hypertensive rats. (nih.gov)
  • Moxonidine is a second-generation centrally acting antihypertensive drug that exhibits high binding affinity for I1 imidazoline receptor subtype. (gov.rs)
  • Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of mild to moderate essential hypertension. (wikipedia.org)
  • Concomitant administration of moxonidine and a thiazide diuretic such as hydrochlorothiazide gave a synergistic antihypertensive effect. (wikipedia.org)
  • Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). (wikipedia.org)
  • Compared to the older central-acting antihypertensives, moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor. (wikipedia.org)
  • Moxonidine is used in the therapy of essential hypertension. (gov.rs)
  • In addition, moxonidine may also promote sodium excretion, improve insulin resistance and glucose tolerance and protect against hypertensive target organ damage, such as kidney disease and cardiac hypertrophy. (wikipedia.org)
  • Moxonidine has an affinity for I1 that is 33 times greater than α2, compared to clonidine which is only four times greater. (wikipedia.org)
  • 3 H]UK4,304 binds to the α 2A receptor of human platelet membranes with high and low affinity K d values of 2.6 and 170 nM, respectively with 73% bound at the high affinity site [ 35 ]. (guidetopharmacology.org)
  • The approved drug oxymetazoline has been mapped to the primary targets α 1A and α 2A adrenoceptors as these have comparably the highest affinity interaction with the drug. (guidetopharmacology.org)
  • As the endogenous ligand, (-)-adrenaline has intrinsic activity across the adrenoceptor family, but we've only tagged α 1D and α 2A subtypes as primary drug target as the drug has highest affinity at these isoforms. (guidetopharmacology.org)
  • However, the data relating to the determination of moxonidine in pharmaceutical dosage forms, in the presence of its organic impurities as well as its potential degradation products, are not yet available. (gov.rs)
  • Routine toxicology studies have provided no evidence that moxonidine has any teratogenic, mutagenic or carcinogenic potential. (wikipedia.org)
  • The development of new, rapid and routinely applicable isocratic RP-HPLC method would significantly improve the qualitative and quantitative analysis of moxonidine in the presence of its impurities in the active pharmaceutical substances and pharmaceutical dosage form. (gov.rs)