Приказ основних података о документу
Imidazoline receptors ligands
Ligandi imidazolinskih receptora
dc.creator | Nikolić, Katarina | |
dc.creator | Agbaba, Danica | |
dc.date.accessioned | 2019-09-02T11:30:30Z | |
dc.date.available | 2019-09-02T11:30:30Z | |
dc.date.issued | 2012 | |
dc.identifier.issn | 0367-598X | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/1764 | |
dc.description.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 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.abstract | 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. 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.publisher | Savez hemijskih inženjera, Beograd | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172033/RS// | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.source | Hemijska industrija | |
dc.subject | I1-Imidazoline receptors | en |
dc.subject | I2-Imidazoline receptors | en |
dc.subject | I3-Imidazolinereceptors | en |
dc.subject | á2-Adrenergic receptors | en |
dc.subject | QSAR | en |
dc.subject | pharmacophores | en |
dc.subject | rilmenidine | en |
dc.subject | clonidine | en |
dc.subject | hypertension | en |
dc.subject | centrallyacting antihypertensives | en |
dc.subject | analgetics | en |
dc.subject | antidiabetics | en |
dc.subject | imidazolinski receptori | sr |
dc.subject | alfa2-adrenergički receptori | sr |
dc.subject | QSAR | sr |
dc.subject | farmakofore | sr |
dc.subject | rilmenidin | sr |
dc.subject | klonidin | sr |
dc.subject | centralni antihipertenzivi | sr |
dc.subject | analgetici | sr |
dc.subject | antidiabetici | sr |
dc.title | Imidazoline receptors ligands | en |
dc.title | Ligandi imidazolinskih receptora | sr |
dc.type | article | |
dc.rights.license | BY-NC-ND | |
dcterms.abstract | Николић, Катарина; Aгбаба, Даница; Лиганди имидазолинских рецептора; Лиганди имидазолинских рецептора; | |
dc.citation.volume | 66 | |
dc.citation.issue | 5 | |
dc.citation.spage | 619 | |
dc.citation.epage | 635 | |
dc.citation.other | 66(5): 619-635 | |
dc.citation.rank | M23 | |
dc.identifier.wos | 000314735800001 | |
dc.identifier.doi | 10.2298/HEMIND120221037N | |
dc.identifier.scopus | 2-s2.0-84869470741 | |
dc.identifier.fulltext | https://farfar.pharmacy.bg.ac.rs//bitstream/id/575/1762.pdf | |
dc.type.version | publishedVersion |