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Imidazoline receptors ligands

Ligandi imidazolinskih receptora

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2012
1762.pdf (441.7Kb)
Authors
Nikolić, Katarina
Agbaba, Danica
Article (Published version)
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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.
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 odno...si 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.

Keywords:
I1-Imidazoline receptors / I2-Imidazoline receptors / I3-Imidazolinereceptors / á2-Adrenergic receptors / QSAR / pharmacophores / rilmenidine / clonidine / hypertension / centrallyacting antihypertensives / analgetics / antidiabetics / imidazolinski receptori / alfa2-adrenergički receptori / QSAR / farmakofore / rilmenidin / klonidin / centralni antihipertenzivi / analgetici / antidiabetici
Source:
Hemijska industrija, 2012, 66, 5, 619-635
Publisher:
  • Savez hemijskih inženjera, Beograd
Funding / projects:
  • Synthesis, Quantitative Structure and Activity Relationship, Physico-Chemical Characterisation and Analysis of Pharmacologically Active Substances (RS-172033)

DOI: 10.2298/HEMIND120221037N

ISSN: 0367-598X

WoS: 000314735800001

Scopus: 2-s2.0-84869470741
[ Google Scholar ]
1
1
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/1764
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Nikolić, Katarina
AU  - Agbaba, Danica
PY  - 2012
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1764
AB  - 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.
AB  - 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.
PB  - Savez hemijskih inženjera, Beograd
T2  - Hemijska industrija
T1  - Imidazoline receptors ligands
T1  - Ligandi imidazolinskih receptora
VL  - 66
IS  - 5
SP  - 619
EP  - 635
DO  - 10.2298/HEMIND120221037N
ER  - 
@article{
author = "Nikolić, Katarina and Agbaba, Danica",
year = "2012",
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., 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.",
publisher = "Savez hemijskih inženjera, Beograd",
journal = "Hemijska industrija",
title = "Imidazoline receptors ligands, Ligandi imidazolinskih receptora",
volume = "66",
number = "5",
pages = "619-635",
doi = "10.2298/HEMIND120221037N"
}
Nikolić, K.,& Agbaba, D.. (2012). Imidazoline receptors ligands. in Hemijska industrija
Savez hemijskih inženjera, Beograd., 66(5), 619-635.
https://doi.org/10.2298/HEMIND120221037N
Nikolić K, Agbaba D. Imidazoline receptors ligands. in Hemijska industrija. 2012;66(5):619-635.
doi:10.2298/HEMIND120221037N .
Nikolić, Katarina, Agbaba, Danica, "Imidazoline receptors ligands" in Hemijska industrija, 66, no. 5 (2012):619-635,
https://doi.org/10.2298/HEMIND120221037N . .

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