The discovery of imidazoline ligands has opened up a new field of study. The investigation of imidazoline actions independent of adrenoceptors started in the mid 1980s. Imidazoline receptors are classified in several subtypes, I1, I2 and I3 binding sites. Although imidazoline sites have been the subjects of research for several years, but there is still controversy about their actions especiall...

The discovery of imidazoline ligands has opened up a new field of study. The investigation of imidazoline actions independent of adrenoceptors started in the mid 1980s. Imidazoline receptors are classified in several subtypes, I1, I2 and I3 binding sites. Although imidazoline sites have been the subjects of research for several years, but there is still controversy about their actions especiall...

The selectivity of tizanidine to the imidazoline-receptor and alpha 2-adrenoceptor recognized by 3H-p-aminoclonidine was examined in rat kidney membranes and was compared with those of other imidazoline compounds. Tizanidine bound to the imidazoline-receptors with approximately 20 times higher affinity than the alpha 2-adrenoceptors. The order of relative selectivity to imidazoline receptor was...

The imidazoline system (a concept which is barely over decades old) consists in imidazoline receptors I, I2 and I3 and their active endogenous ligands, the most important of which is agmatine. Brain contains both I1 and 12 of imidazoline receptors. One of the most important functions of this system is modulation of different behaviour components, such as suicidal behaviour, stress, anxiety, foo...

Monoamine oxidase B (MAO-B) was recently identified as a member of the family of imidazoline binding proteins. To localize the imidazoline binding domain on MAO-B, we labeled the domain with the imidazoline photoaffinity adduct [I]2-(3azido-4-iodophenoxy)methylimidazoline in rat and human liver and visualized labeled peptides by autoradiography/sodium dodecyl sulfate-polyacrylamide gel electrop...

Monoamine oxidase B (MAO-B) was recently identified as a member of the family of imidazoline binding proteins. To localize the imidazoline binding domain on MAO-B, we labeled the domain with the imidazoline photoaffinity adduct [125I]2-(3-azido-4-iodophenoxy)methylimidazoline in rat and human liver and visualized labeled peptides by autoradiography/sodium dodecyl sulfate-polyacrylamide gel elec...

properties of agmatine and endogenous clonidine-displacing substance at imidazoline and alpha-2 adrenergic receptors. A. Imidazoline-guanidinium receptive site in renal proximal tubule: asymmetric distribution, regulation by cations and interaction with an endogenous clonidine displacing substance.idazoxan label different populations of imidazoline sites on rat kidney.

Administration (3 to 100 microg/kg IV) of clonidine, rilmenidine, and an imidazoline derivative, 2-(2-chlorophenylamino)imidazoline, in pithed nonstimulated rabbits caused a dose-dependent increase in mean arterial pressure without affecting heart rate. Prazosin (0.1 mg/kg IV) almost abolished the pressor responses to 2-(2-chlorophenylamino)imidazoline, partially inhibited those induced by clon...

Imidazoline receptors are expressed widely in the CNS. In the present study, whole-cell patch-clamp recordings were made from medium spiny neurons in dorsal striatum slices from the rat brain, and the roles of I1-imidazoline receptors in the modulation of synaptic transmission were studied. Moxonidine, an I1-imidazoline receptor agonist, decreased the GABAA receptor-mediated IPSCs in a concentr...

Since 20 years the concept of specific imidazoline receptors has remained controversial. The problem with imidazoline receptors is mostly due to their functional similarity to alpha-adrenoceptors. In this work, a pharmacodynamic model of isolated rat jejunum longitudinal muscle strips constricted with acetylcholine (Ach) was applied to separate functional properties of the two types of receptor...