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Imidazoline Antihypertensive Drugs: Selective I1-Imidazoline Receptors Activation

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2012
1733.pdf (496.3Kb)
Authors
Nikolić, Katarina
Agbaba, Danica
Article (Published version)
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Abstract
Involvement of imidazoline receptors (IR) in the regulation of vasomotor tone as well as in the mechanism of action of some centrally acting antihypertensives has received tremendous attention. To date, pharmacological studies have allowed the characterization of three main imidazoline receptor classes, the I1-imidazoline receptor which is involved in central inhibition of sympathetic tone to lower blood pressure, the I2-imidazoline receptor which is an allosteric binding site of monoamine oxidase B (MAO-B), and the I3-imidazoline receptor which regulates insulin secretion from pancreatic beta-cells. All three imidazoline receptors represent important targets for cardiovascular research. The hypotensive effect of clonidine-like centrally acting antihypertensives was attributed both to a2-adrenergic receptors and nonadrenergic I1-imidazoline receptors, whereas their sedative action involves activation of only a2-adrenergic receptors located in the locus coeruleus. Since more selective I...1-imidazoline receptors ligands reduced incidence of typical side effects of other centrally acting antihypertensives, there is significant interest in developing new agents with higher selectivity and affinity for I1-imidazoline receptors. The selective imidazoline receptors agents are also more effective in regulation of body fat, neuroprotection, inflammation, cell proliferation, epilepsy, depression, stress, cell adhesion, and pain. New agonists and antagonists with high selectivity for imidazoline receptor subtypes 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 theoretical studies of imidazoline receptor ligands.

Keywords:
a2-Adrenergic receptors / Centrally acting antihypertensives / Clonidine / Hypertension / Imidazoline receptors / Rilmenidine
Source:
Cardiovascular Therapeutics, 2012, 30, 4, 209-216
Publisher:
  • Wiley, Hoboken
Funding / projects:
  • Synthesis, Quantitative Structure and Activity Relationship, Physico-Chemical Characterisation and Analysis of Pharmacologically Active Substances (RS-172033)

DOI: 10.1111/j.1755-5922.2011.00269.x

ISSN: 1755-5914

PubMed: 21884004

WoS: 000305942100008

Scopus: 2-s2.0-84863219482
[ Google Scholar ]
28
26
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/1735
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/123456789/1735
AB  - Involvement of imidazoline receptors (IR) in the regulation of vasomotor tone as well as in the mechanism of action of some centrally acting antihypertensives has received tremendous attention. To date, pharmacological studies have allowed the characterization of three main imidazoline receptor classes, the I1-imidazoline receptor which is involved in central inhibition of sympathetic tone to lower blood pressure, the I2-imidazoline receptor which is an allosteric binding site of monoamine oxidase B (MAO-B), and the I3-imidazoline receptor which regulates insulin secretion from pancreatic beta-cells. All three imidazoline receptors represent important targets for cardiovascular research. The hypotensive effect of clonidine-like centrally acting antihypertensives was attributed both to a2-adrenergic receptors and nonadrenergic I1-imidazoline receptors, whereas their sedative action involves activation of only a2-adrenergic receptors located in the locus coeruleus. Since more selective I1-imidazoline receptors ligands reduced incidence of typical side effects of other centrally acting antihypertensives, there is significant interest in developing new agents with higher selectivity and affinity for I1-imidazoline receptors. The selective imidazoline receptors agents are also more effective in regulation of body fat, neuroprotection, inflammation, cell proliferation, epilepsy, depression, stress, cell adhesion, and pain. New agonists and antagonists with high selectivity for imidazoline receptor subtypes 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 theoretical studies of imidazoline receptor ligands.
PB  - Wiley, Hoboken
T2  - Cardiovascular Therapeutics
T1  - Imidazoline Antihypertensive Drugs: Selective I1-Imidazoline Receptors Activation
VL  - 30
IS  - 4
SP  - 209
EP  - 216
DO  - 10.1111/j.1755-5922.2011.00269.x
ER  - 
@article{
author = "Nikolić, Katarina and Agbaba, Danica",
year = "2012",
abstract = "Involvement of imidazoline receptors (IR) in the regulation of vasomotor tone as well as in the mechanism of action of some centrally acting antihypertensives has received tremendous attention. To date, pharmacological studies have allowed the characterization of three main imidazoline receptor classes, the I1-imidazoline receptor which is involved in central inhibition of sympathetic tone to lower blood pressure, the I2-imidazoline receptor which is an allosteric binding site of monoamine oxidase B (MAO-B), and the I3-imidazoline receptor which regulates insulin secretion from pancreatic beta-cells. All three imidazoline receptors represent important targets for cardiovascular research. The hypotensive effect of clonidine-like centrally acting antihypertensives was attributed both to a2-adrenergic receptors and nonadrenergic I1-imidazoline receptors, whereas their sedative action involves activation of only a2-adrenergic receptors located in the locus coeruleus. Since more selective I1-imidazoline receptors ligands reduced incidence of typical side effects of other centrally acting antihypertensives, there is significant interest in developing new agents with higher selectivity and affinity for I1-imidazoline receptors. The selective imidazoline receptors agents are also more effective in regulation of body fat, neuroprotection, inflammation, cell proliferation, epilepsy, depression, stress, cell adhesion, and pain. New agonists and antagonists with high selectivity for imidazoline receptor subtypes 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 theoretical studies of imidazoline receptor ligands.",
publisher = "Wiley, Hoboken",
journal = "Cardiovascular Therapeutics",
title = "Imidazoline Antihypertensive Drugs: Selective I1-Imidazoline Receptors Activation",
volume = "30",
number = "4",
pages = "209-216",
doi = "10.1111/j.1755-5922.2011.00269.x"
}
Nikolić, K.,& Agbaba, D.. (2012). Imidazoline Antihypertensive Drugs: Selective I1-Imidazoline Receptors Activation. in Cardiovascular Therapeutics
Wiley, Hoboken., 30(4), 209-216.
https://doi.org/10.1111/j.1755-5922.2011.00269.x
Nikolić K, Agbaba D. Imidazoline Antihypertensive Drugs: Selective I1-Imidazoline Receptors Activation. in Cardiovascular Therapeutics. 2012;30(4):209-216.
doi:10.1111/j.1755-5922.2011.00269.x .
Nikolić, Katarina, Agbaba, Danica, "Imidazoline Antihypertensive Drugs: Selective I1-Imidazoline Receptors Activation" in Cardiovascular Therapeutics, 30, no. 4 (2012):209-216,
https://doi.org/10.1111/j.1755-5922.2011.00269.x . .

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