Naphazoline-induced Suppression of Aqueous Humor Pressure and Flow: Involvement of Central and Peripheral α2/I1Receptors

Ogidigben, Miller J.; Chu, Teh-Ching; Potter, David E.

doi:10.1006/exer.2000.0960

Cited by 8 publications

(6 citation statements)

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“…These so-called I 1 receptors have been characterized by binding studies (Molderings et al, 1993;Piletz et al, 1996;Ernsberger et al, 1997) and by cellular (Separovic et al, 1996;Greney et al, 2000) and "in vivo" effects (Bousquet et al, 1984;Ernsberger et al, 1990;Smyth and Penner, 1999;Bruban et al, 2001;Ogidigben et al, 2001). At the time, the available radioligands, used to perform binding studies on the I 1 R, exhibit low selectivity versus ␣ 2 AR (Molderings et al, 1993;Piletz et al, 1996;Ernsberger et al, 1997).…”

Section: Discussionmentioning

confidence: 99%

“…Moreover, pharmacological studies have shown that this receptor is involved in several functions such as regulation of the cardiovascular function (Bousquet et al, 1984;Ernsberger et al, 1990), modulation of the ocular pressure (Ogidigben et al, 2001), control of the catecholamine release from chromaffin cells (Nguyen and De Lean, 1987), and renal sodium excretion (Smyth and Penner, 1999).…”

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confidence: 99%

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[¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁Imidazoline Receptors

Greney¹,

Urosevic²,

Schann³

et al. 2002

Mol Pharmacol

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The I 1 subtype of imidazoline receptors (I 1 R) is a plasma membrane protein that is involved in diverse physiological functions. Available radioligands used so far to characterize the I 1 R were able to bind with similar affinities to ␣ 2 -adrenergic receptors (␣ 2 -ARs) and to I 1 R. This feature was a major drawback for an adequate characterization of this receptor subtype. New imidazoline analogs were therefore synthesized and the present study describes one of these compounds, 2-(2-chloro-4-iodophenylamino)-5-methyl-pyrroline (LNP 911), which was of high affinity and selectivity for the I 1 R. LNP 911 was radioiodinated and its binding properties characterized in different membrane preparations. Saturation experiments with [

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

[¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁Imidazoline Receptors

Greney¹,

Urosevic²,

Schann³

et al. 2002

Mol Pharmacol

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“…In ophthalmology, naphazoline side effects include blurred vision, irritation, mydriasis, increased or decreased intraocular pressure [23]. In addition, an experiment in rabbit eye showed a reduced aqueous humor flow rate in the eye chamber [30]. Further experimental studies have shown that naphazoline topical application in rabbit eye leads to an increase of endogenous atrial natriuretic peptide and decrease of noradrenaline in the cornea, and significantly increased cyclic nucleotides (cAMP, cGMP) through interaction with imidazoline receptors [29].…”

Section: Current Issues In Pharmacy and Medical Sciencesmentioning

confidence: 99%

Rationale for naphazoline effects in-depth study

Kuzminov

Turkina

Кuzminov

2018

Current Issues in Pharmacy and Medical Sciences

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This article presents a retrospective review of data on side effects of drugs containing naphazoline and data on toxicity of the agent when entered the body via different pathways. Most publications on clinical signs of possible naphazoline-associated side effects are lacking thorough analysis of possible causes. Limited data on the pharmacokinetics and pharmacodynamics of the drug led to various complications after its administration. Therefore, further studies on naphazoline content dynamics or products of its biotransformation in biological substrates and determination of half-life of the agent must be conducted. This will allow establishingsafe levels for different exposure pathways and harmful levels of the naphazoline with respect to its material accumulation. It should be noted that scientific publications contain controversial data regarding allergenic potential of the agent. Possible side effects of the drug on the reproductionand development are not revealed. Determination of effects the products containing naphazoline may have on immune and reproductive system is an important part of the research.

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“…On the other hand, pharmacological studies have shown that I 1 ‐imidazoline receptors are involved in several functions such as regulation of the cardiovascular function [1,3], modulation of the ocular pressure [56], renal sodium excretion [57], and control of the catecholamine release from chromaffin cells [58].…”

Section: I1‐imidazoline Receptor Ligandsmentioning

confidence: 99%

Imidazoline Antihypertensive Drugs: Selective I₁‐Imidazoline Receptors Activation

Nikolic

Agbaba

2011

Cardiovascular Therapeutics

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SUMMARYInvolvement 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 I 1 -imidazoline receptor which is involved in central inhibition of sympathetic tone to lower blood pressure, the I 2 -imidazoline receptor which is an allosteric binding site of monoamine oxidase B (MAO-B), and the I 3 -imidazoline receptor which regulates insulin secretion from pancreatic β-cells. All three imidazoline receptors represent important targets for cardiovascular research. The hypotensive effect of clonidine-like centrally acting antihypertensives was attributed both to α 2 -adrenergic receptors and nonadrenergic I 1 -imidazoline receptors, whereas their sedative action involves activation of only α 2 -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 I 1 -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.

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Naphazoline-induced Suppression of Aqueous Humor Pressure and Flow: Involvement of Central and Peripheral α2/I1Receptors

Cited by 8 publications

References 20 publications

[¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁Imidazoline Receptors

[¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁Imidazoline Receptors

Rationale for naphazoline effects in-depth study

Imidazoline Antihypertensive Drugs: Selective I₁‐Imidazoline Receptors Activation

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Naphazoline-induced Suppression of Aqueous Humor Pressure and Flow: Involvement of Central and Peripheral α2/I1Receptors

Cited by 8 publications

References 20 publications

[125I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I1Imidazoline Receptors

[125I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I1Imidazoline Receptors

Rationale for naphazoline effects in-depth study

Imidazoline Antihypertensive Drugs: Selective I1‐Imidazoline Receptors Activation

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[¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁Imidazoline Receptors

[¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁Imidazoline Receptors

Imidazoline Antihypertensive Drugs: Selective I₁‐Imidazoline Receptors Activation