Abstract
Extensive biochemical and pharmacological studies have determined three different subtypes of imidazoline receptors: I1-imidazoline receptors (I1-IR) involved in central inhibition of sympathicus that produce hypotensive effect; I2-imidazoline receptors (I2-IR) modulate monoamine oxidase B activity (MAO-B); I3-imidazoline receptors (I3-IR) regulate insulin secretion from pancreatic ?-cells. Therefore, the I1/I2/I3 imidazoline receptors are selected as new, interesting targets for drug design and discovery. Novel selective I1/I2/I3 agonists and antagonists have been recently developed. In the present review, we provide a brief update to the field of imidazoline research, highlighting some of the chemical diversity and progress made in the 2D-QSAR, 3D-QSAR and quantitative pharmacophore development studies of I1-IR and I2-IR imidazoline receptor ligands. Theoretical studies of I3-IR ligands are not yet performed because of insufficient number of synthesized I3-IR ligands.
Highlights
In the present review, we provide a brief update to the field of imidazoline research, highlighting some of the chemical diversity and progress made in the 2D-QSAR, 3D-QSAR and quantitative pharmacophore development studies of I1-imidazolinski receptori (I1-Imidazolinski receptori (IR)) and I2-imidazolinski receptori (I2-IR) imidazoline receptor ligands
Study of retention parameters obtained in RP-TLC system and their application on QSAR/QSPR of some alpha adrenergic and imidazoline receptor ligands, J
Summary
Izvod Imidazolinski receptori (IR) na osnovu farmakološkog efekta podeljeni su u tri osnovne klase: I1-imidazolinski receptori (I1-IR) – učestvuju u centralnoj inhibiciji simpatikusa koja prouzrokuje sniženje krvnog pritiska; I2-imidazolinski receptori (I2-IR) – predstavljaju alosterno mesto vezivanja monoamino oksidaze B (MAO-B) i I3-imidazolinski receptori (I3-IR) – regulišu sekreciju insulina iz β-ćelija pankreasa. Zbog svoje uloge u organizmu sve tri klase imidazolinskih receptora predstavljaju veoma važno ciljno mesto za istraživanja novih lekova. Zato su prethodnih godina veoma intenzivno izučavani farmakološki efekti aktivacije I1-IR, I2-IR i I3-IR podtipova imidazolinskih receptora i njihova povezanost sa aktivacijom drugih signalnih puteva. U ovom preglednom radu biće prikazani glavni odnosi između afiniteta ka specifičnim podtipovima imidazolinskih receptora (I1-IR i I2-IR) i strukture liganada, ispitivani pomoću 2D-QSAR (quantitative structure–activity relationship) studija, 3D --QSAR studija i analize 3D-strukture farmakofore. Ključne reči: imidazolinski receptori; alfa2-adrenergički receptori; QSAR; farmakofore; rilmenidin; klonidin; centralni antihipertenzivi; analgetici; antidiabetici
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