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Ligandi imidazolinskih receptora

dc.creatorNikolić, Katarina
dc.creatorAgbaba, Danica
dc.date.accessioned2019-09-02T11:30:30Z
dc.date.available2019-09-02T11:30:30Z
dc.date.issued2012
dc.identifier.issn0367-598X
dc.identifier.urihttps://farfar.pharmacy.bg.ac.rs/handle/123456789/1764
dc.description.abstractExtensive 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 β-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 recently been 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 have not yet been performed because of insufficient number of synthesized I3-IR ligands.en
dc.description.abstractImidazolinski 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. Nedavno sintetisani i ispitani visokoselektivni agonisti i antagonisti I1- -IR i I2-IR, omogućili su izvođenje detaljnijih teorijskih studija radi definisanja osnovnih farmakofora ovih liganada. 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.sr
dc.publisherSavez hemijskih inženjera, Beograd
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172033/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/
dc.sourceHemijska industrija
dc.subjectI1-Imidazoline receptorsen
dc.subjectI2-Imidazoline receptorsen
dc.subjectI3-Imidazolinereceptorsen
dc.subjectá2-Adrenergic receptorsen
dc.subjectQSARen
dc.subjectpharmacophoresen
dc.subjectrilmenidineen
dc.subjectclonidineen
dc.subjecthypertensionen
dc.subjectcentrallyacting antihypertensivesen
dc.subjectanalgeticsen
dc.subjectantidiabeticsen
dc.subjectimidazolinski receptorisr
dc.subjectalfa2-adrenergički receptorisr
dc.subjectQSARsr
dc.subjectfarmakoforesr
dc.subjectrilmenidinsr
dc.subjectklonidinsr
dc.subjectcentralni antihipertenzivisr
dc.subjectanalgeticisr
dc.subjectantidiabeticisr
dc.titleImidazoline receptors ligandsen
dc.titleLigandi imidazolinskih receptorasr
dc.typearticle
dc.rights.licenseBY-NC-ND
dcterms.abstractНиколић, Катарина; Aгбаба, Даница; Лиганди имидазолинских рецептора; Лиганди имидазолинских рецептора;
dc.citation.volume66
dc.citation.issue5
dc.citation.spage619
dc.citation.epage635
dc.citation.other66(5): 619-635
dc.citation.rankM23
dc.identifier.wos000314735800001
dc.identifier.doi10.2298/HEMIND120221037N
dc.identifier.scopus2-s2.0-84869470741
dc.identifier.fulltexthttps://farfar.pharmacy.bg.ac.rs//bitstream/id/575/1762.pdf
dc.type.versionpublishedVersion


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