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1 General aspects (0)   1.1 Epidemiology (19)   1.2 Population genetics (0)   1.3 Pathogenesis (3)   1.4 Quality of life (4)   1.5 Glaucomas as cause of blindness (9)   1.6 Prevention and screening (8) 2 Anatomical structures in glaucoma (0)   2.1 Conjunctiva (4)   2.2 Cornea (22)   2.3 Sclera (2)   2.4 Anterior chamber angle (2)   2.5 Meshwork (0)     2.5.1 Trabecular meshwork (8)     2.5.2 Schlemms canal (0)     2.5.3 Scleral outlet channels (0)   2.6 Aqueous humor dynamics (0)     2.6.1 Production (0)     2.6.2 Outflow (1)       2.6.2.1 Trabecular meshwork (1)       2.6.2.2 Uveoscleral (0)     2.6.3 Compostion (1)   2.7 Episcleral veins and venous pressure (0)   2.8 Iris (6)   2.9 Ciliary body (0)   2.10 Lens (0)   2.11 Vitreous body (0)   2.12 Choroid, peripapillary choroid, peripapillary atrophy (5)   2.13 Retina and retinal nerve fibre layer (9)   2.14 Optic disc (11)   2.15 Optic nerve (3)   2.16 Chiasma and retrochiasmal central nervous system (6)   2.17 Stem cells (2)   2.20 Other (0) 3 Laboratory methods (0)   3.1 Microscopy (2)   3.2 Electron microscopy (1)   3.3 Immunohistochemistry (2)   3.4 Molecular genetics (0)     3.4.1 Linkage studies (1)     3.4.2 Gene studies (29)   3.5 Molecular biology incl. SiRNA (7)   3.6 Cellular biology (17)   3.7 Biochemistry (1)   3.8 Pharmacology (5)   3.9 Pathophysiology (2)   3.10 Immunobiology (2)   3.11 Pharmacogenetics (0)   3.12 Proteomics (1)   3.13 In vivo imaging (0)     3.13.1 Laser Scanning (0)       3.13.1.1 Confocal Scanning Laser Ophthalmoscopy (1)       3.13.1.2 Confocal Scanning Laser Polarimetry (1)     3.13.2 Optical Coherence Tomography (0)       3.13.2.1 Anterior Segment (0)       3.13.2.2 Posterior Segment (0)     3.13.3 RGC Imaging (0)     3.13.4 Other (0)   3.20 Other (0) 4 Tissue culture of ocular cells (0) 5 Experimental glaucoma; animal models (2)   5.1 Rodent (17)   5.2 Primates (4)   5.3 Other (8) 6 Clinical examination methods (0)   6.1 Intraocular pressure measurement; factors affecting IOP (0)     6.1.1 Devices, techniques (5)     6.1.2 Fluctuation, circadian rhythms (5)     6.1.3 Factors affecting IOP (10)   6.2 Tonography, aqueous flow measurement (see also 2.6) (2)   6.3 Biomicroscopy (slitlamp) (0)     6.3.1 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associated with intraocular tumors (5)     9.4.9 Glaucomas associated with elevated episcleral venous pressure (0)       9.4.10 Glaucomas associated with hemorrhage (0)     9.4.11 Glaucomas following intraocular surgery (1)       9.4.11.1 Ciliary block (malignant) glaucoma (1)       9.4.11.2 Glaucomas in aphakia and pseudophakia (3)       9.4.11.3 Epithelial, fibrous, and endothelial proliferation (0)       9.4.11.4 Glaucomas associated with corneal surgery (10)       9.4.11.5 Glaucomas associated with vitreoretinal surgery (3)     9.4.15 Glaucoma in relation to systemic disease (27)     9.4.20 Other (2) 10 Differential diagnosis e.g. anterior and posterior ischemic optic neuropathy (4) 11 Medical treatment (0)   11.1 General management, indication (1)   11.2 Cholinergic drugs (3)   11.3 Adrenergic drugs (0)     11.3.1 Epinephrine (0)     11.3.2 Thymoxamine, dapiprazole (0)     11.3.3 Apraclonidine, brimonidine (0)     11.3.4 Betablocker (4)     11.3.5 Other (0)   11.4 Prostaglandins 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    12.8.1 Without tube implant (9)     12.8.2 With tube implant or other drainage devices (18)     12.8.3 Non-perforating (5)     12.8.4 Using laser (0)     12.8.5 Other (0)     12.8.10 Woundhealing antifibrosis (8)     12.8.11 Complications, endophthalmitis (3)   12.9 Trabeculotomy, goniotomy (7)   12.10 Cyclodestruction (3)   12.11 Cyclodialysis (0)   12.12 Cataract extraction (0)     12.12.1 Intracapsular (0)     12.12.2 Extracapsular (0)     12.12.3 Phacoemulsification (6)   12.14 Combined cataract extraction and glaucoma surgery (0)     12.14.1 Intracapsular (0)     12.14.2 Extracapsular (0)     12.14.3 Phacoemulsification (10)   12.15 Capsulotomy (0)   12.16 Vitrectomy (0)   12.17 Anesthesia (4)   12.20 Other (2) 13 Therapeutic prognosis and outcome (0)   13.1 Prognostic factors (1)   13.2 Outcome (0)     13.2.1 IOP (0)     13.2.2 Visual field (0)       13.2.2.1 Progression (0)       13.2.2.2 Improvement (0)     13.2.3 Other (0) 14 Costing studies; pharmacoeconomics (3) 15 Miscellaneous (20)

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Abstract #50553 Published in IGR 14-2

Update in glaucoma medicinal chemistry: emerging evidence for the importance of melatonin analogues

Crooke A; Colligris B; Pintor J
Current Medicinal Chemistry 2012; 19: 3508-3522

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Glaucoma is a chronic progressive optic neuropathy, which can result in visual impairment and blindness. Elevated intraocular pressure (IOP) is currently the only modifiable risk factor. Several recent studies have shown the benefits of IOP reduction in open-angle glaucoma. Therefore, current glaucoma drugs are IOP-lowering substances such as α2-adrenergic agonists, β2-adrenergic antagonists, carbonic anhydrase inhibitors and hypotensive lipids, which are used separately or in combination. In spite of the wide variety of antiglaucoma medicines, all therapies have several undesirable side effects. As a consequence, there are constant research attempts on the discovery of novel ocular hypotensive drugs. In the current paper, we review the latest available patents and literature for the pharmacological treatment of glaucoma, focusing on their molecular targets and/or their chemical characteristics and especially directed to melatoninergic drugs. Melatonin is a hormone secreted into the blood mainly from the pineal gland allowing the entrainment of the circadian rhythms of several biological functions. Melatonin and its analogues potently reduce IOP in rabbits, monkeys and humans. In addition, there are indications of long-term hypotensive effects and a proven neuroprotective role of melatoninergic substances. Furthermore, antidepressant and normalizing circadian rhythm actions of melatonin analogues might be beneficial for glaucoma patients. All the above mentioned facts suggest these agents as proper candidates for the glaucoma treatment. Consequently, the scientific research has given new and significant progress on the development of new, potent and selective melatonin ligands.

Departamento de Bioquimica y Biologia Molecular IV, E.U. Optica, Universidad Complutense de Madrid, C/Arcos de Jalon 118, 28037 Madrid, Spain. jpintor@vet.ucm.es.

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Classification:

11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)

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