BACKGROUND A downregulation of I(2)-imidazoline binding sites has been reported in frontal cortices of depressed suicide victims, according to I(2)-radioligand binding and confirmed by Western blotting. We now report Western blots of imidazoline receptor proteins in hippocampi of subjects with and without depression at the time of death. METHODS Postmortem diagnoses were obtained from 17 case...

BACKGROUND Dexmedetomidine (Precedex; Abbott Laboratories, Abbott Park, IL) is a selective alpha2-adrenergic agonist that also has affinity for imidazoline receptors. In clinical studies, dexmedetomidine has sedative effects and impairs memory, but the action of dexmedetomidine on synaptic plasticity in the brain has yet to be established. In the present study, the authors investigated the effe...

In the title compound, C(15)H(21)N(2)O(5), the imidazoline ring displays a twisted conformation. The mean plane of the imidazoline ring makes a dihedral angle of 22.55 (5)° with the benzene ring. In the crystal, O-H⋯O and C-H⋯O hydrogen bonds link the mol-ecules into a layer parallel to the bc plane.

The compound 2-(2-benzofuranyl)-2-imidazoline (2-BFI) is a 2-imidazoline derivative that selectively inhibits the in vitro activity of monoamine oxidase-A and it is also an imidazoline I(2) agonist. However, the antidepressant potential of this compound and its mechanism of action have not been well defined. Therefore, in this study we investigated the antidepressant-like effect of 2-BFI in mic...

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...

Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a-k inspired by 2-BFI scaffold to assess imidazoline molecules as D(2)-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided pa...

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...