In this study using clonidine (a mixed ?2 /I1 receptors agonist), tizanidine (pure ?2-receptor agonist), rilmenidine (I1 receptor agonist) and yohimbine (?2-receptor antagonist), we tried to clarify the role of imidazoline and ?2-receptors in morphine withdrawal syndrome. Morphine-dependence was induced by administration of increasing doses of morphine in mice. After the last administration of ...

In this study using clonidine (a mixed ?2 /I1 receptors agonist), tizanidine (pure ?2-receptor agonist), rilmenidine (I1 receptor agonist) and yohimbine (?2-receptor antagonist), we tried to clarify the role of imidazoline and ?2-receptors in morphine withdrawal syndrome. Morphine-dependence was induced by administration of increasing doses of morphine in mice. After the last administration of ...

Large doses of the imidazoline alpha 2 adrenoreceptor agonist clonidine aggravate ethanol-induced gastric lesions. The alpha 2 adrenoceptor antagonist phentolamine, the opioid antagonist naloxone and the H2 antagonist cimetidine do not prevent this action of clonidine suggesting that it is not mediated by alpha 2, opioid or H2 receptors. Further, like clonidine, high doses of phentolamine and c...

Clonidine, moxonidine, and rilmenidine are centrally acting antihypertensive agents that lower arterial pressure by inhibiting the tonic activity of sympathoexcitatory neurons in the rostral ventrolateral medulla. Competing hypotheses have been put forward by different investigators to explain the sympathoinhibition evoked by "imidazoline drugs": either via central actions at α2-adrenergic rece...

The present study aimed at investigating the influence of imidazoline receptor ligands on the proliferation of PC12 cells and the involvement of the sphingosine-1-phosphate (S1P) signaling system in this effect. In cultured PC12 cells, S1P (0.3-100 nM) and the I(1) imidazoline receptor ligands moxonidine (0.3 and 1 mM), agmatine (1 mM), idazoxan (10-100 microM) and efaroxan (1-100 microM) conce...

In the title compound, C(15)H(21)N(2)O(4), the imidazoline ring displays a twisted conformation. The dihedral angle between the mean plane of the imidazoline ring and the benzene ring is 33.50 (12)°. In the crystal, mol-ecules are connected by O-H⋯O hydrogen bonds, forming a zigzag chain along the c axis. The chains are linked by C-H⋯O and C-H⋯π inter-actions.

Previous studies have shown that a subpopulation of the catecholamine-degrading enzymes monoamine oxidase (MAO) A and B holds a previously unknown regulatory site, the I2-imidazoline binding site (I2BS). In the present work, we characterized the isoforms of monoamine oxidases expressed in the rabbit renal proximal tubule, defined their relationship with I2BS, and investigated the ability of I2B...

1. I1 non-adrenoceptor, imidazoline receptor agonists, such as moxonidine, increase urine flow rate and sodium excretion following infusion into the renal artery. The functions of these agonists in genetic and acquired models of hypertension have not been determined. 2. We therefore studied the renal effects of two known non-adrenoceptor, imidazoline receptor agonists, rilmenidine and moxonidin...

UNLABELLED Discovered in 1984, imidazoline receptors (I1, I2, I3) are located centrally and peripherally being involved in various physiologic and pathophysiologic processes in the body. Experimental and clinical investigations have suggested the interrelations between imidazoline, adrenergic, dopaminergic, glutamatergic and opioid systems, which may explain the influence of different substance...