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Review
. 2021 Aug 11;11(8):1186.
doi: 10.3390/biom11081186.

Novel Insight of Histamine and Its Receptor Ligands in Glaucoma and Retina Neuroprotection

Silvia Sgambellone  1 , Laura Lucarini  1 , Cecilia Lanzi  2 , Emanuela Masini  1
Affiliations
Review

Novel Insight of Histamine and Its Receptor Ligands in Glaucoma and Retina Neuroprotection

Silvia Sgambellone et al. Biomolecules. .

Abstract

Glaucoma is a multifactorial neuropathy characterized by increased intraocular pressure (IOP), and it is the second leading cause of blindness worldwide after cataracts. Glaucoma combines a group of optic neuropathies characterized by the progressive degeneration of retinal ganglionic cells (RGCs). Increased IOP and short-term IOP fluctuation are two of the most critical risk factors in glaucoma progression. Histamine is a well-characterized neuromodulator that follows a circadian rhythm, regulates IOP and modulates retinal circuits and vision. This review summarizes findings from animal models on the role of histamine and its receptors in the eye, focusing on the effects of histamine H3 receptor antagonists for the future treatment of glaucomatous patients.

Keywords: baro-protection; histamine; histamine H3R antagonists; intraocular pressure (IOP).

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Western blot analysis of histamine H1R (A), H3R (B) and H4R (C) subtypes in the retina, ciliary body, optic nerve, and stomach samples of New Zealand White (NZW) rabbits. Densitometric data of 6 determinations are reported as relative optical density, corrected for the corresponding β-actin content [60] modified.
Figure 2
Figure 2
IOP lowering effect of ciproxifan in the transient ocular hypertensive model in NZW rabbits. The effect of ciproxifan is suppressed by pre-treatment with 1% imetit. * p < 0.05 ciproxifan 1% at 60′ and 120′ vs. vehicle and imetit 1% + ciproxifan 1%. All the results are expressed as mean ± SEM (n = 6). Two-way ANOVA followed by Bonferroni post hoc test.
Figure 3
Figure 3
Representative images of hematoxylin/eosin-stained histological sections of retinae from different treated groups. RGCs are visible in the upper layer. The histological sections of Vehicle, Ciproxifan and DL-76 panels were prepared from carbomer-induced glaucoma models in male NZW rabbits with stable elevated IOP [60] modified.
See this image and copyright information in PMC

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