- Insights into divalent cation regulation and G13-coupling of orphan receptor GPR35. [Journal Article]
- Endogenous ions play important roles in the function and pharmacology of G protein-coupled receptors (GPCRs) with limited atomic evidence. In addition, compared with G protein subtypes Gs, Gi/o, and Gq/11, insufficient structural evidence is accessible to understand the coupling mechanism of G12/13 protein by GPCRs. Orphan receptor GPR35, which is predominantly expressed in the gastrointestinal t…
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- Autonomic nervous system receptor-mediated regulation of mast cell degranulation modulates the inflammation after corneal epithelial abrasion. [Journal Article]
- Mast cells (MCs) regulate wound healing and are influenced by the autonomic nervous system (ANS). However, the underlying mechanisms affecting wound healing outcomes remain elusive. Here, we explored the specific role of the ANS by regulating MC degranulation following corneal epithelium abrasion. A mouse model of corneal abrasion was established by mechanically removing a 2-mm central epithelium…
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- Candidates for Repurposing as Anti-Virulence Agents Based on the Structural Profile Analysis of Microbial Collagenase Inhibitors. [Journal Article]
- The pharmacological inhibition of the bacterial collagenases (BC) enzymes is considered a promising strategy to block the virulence of the bacteria without targeting the selection mechanism leading to drug resistance. The chemical structures of the Clostridium perfringens collagenase A (ColA) inhibitors were analyzed using Bemis-Murcko skeletons, Murcko frameworks, the type of plain rings, and do…
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- Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35 [Journal Article]
- A previous pharmacogenomic analysis identified cromolyn, an anti-allergic drug, as an effective anti-fibrotic agent that acts on hepatocytes and stellate cells. Furthermore, cromolyn was shown to be a G protein-coupled receptor 35 (GPR35) agonist. However, it has not been studied whether anti-fibrotic effects are mediated by GPR35. Therefore, in this study, the role of GPR35 in hepatic fibrosis w…
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- Drugs and Lactation Database (LactMed): Lodoxamide [BOOK]Drugs and Lactation Database (LactMed). National Library of Medicine (US): Bethesda (MD)BOOK
- Although no published data exist on the use of lodoxamide during lactation, maternal milk levels are likely to be very low after the use eye drops. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
- Protective effect of lodoxamide on hepatic steatosis through GPR35. [Journal Article]
- Although GPR35 is an orphan G protein-coupled receptor, synthetic agonists and antagonists have been developed. Recently, cromolyn, a mast cell stabilizer, was reported as an agonist of GPR35 and was shown to exhibit antifibrotic effects through its actions on hepatocytes and stellate cells. In this study, the role of GPR35 in hepatic steatosis was investigated using an in vitro model of liver X …
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- GPR35 mediates lodoxamide-induced migration inhibitory response but not CXCL17-induced migration stimulatory response in THP-1 cells; is GPR35 a receptor for CXCL17? [Journal Article]
- CONCLUSIONS: The present findings suggest that GPR35 functions as a migration inhibitory receptor, but CXCL17-stimulated migration of THP-1 cells is not dependent on GPR35.
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- Efficacy and safety of 0.1% lodoxamide for the long-term treatment of superior limbic keratoconjunctivitis. [Journal Article]
- CONCLUSIONS: Lodoxamide 0.1% is an efficacious therapeutic alternative for the treatment of active and chronic SLK. This medication has proved to be safe and well tolerated.
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- Vernal keratoconjunctivitis: a severe allergic eye disease with remodeling changes. [Review]
- Vernal keratoconjunctivitis (VKC) is an unusually severe sight-threatening allergic eye disease, occurring mainly in children. Conventional therapy for allergic conjunctivitis is generally not adequate for VKC. Pediatricians and allergists are often not familiar with the severe clinical symptoms and signs of VKC. As untreated VKC can lead to permanent visual loss, pediatric allergists should be a…
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- The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35. [Journal Article]
- Lack of high potency agonists has restricted analysis of the G protein-coupled receptor GPR35. Moreover, marked variation in potency and/or affinity of current ligands between human and rodent orthologs of GPR35 has limited their productive use in rodent models of physiology. Based on the reported modest potency of the antiasthma and antiallergic ligands cromolyn disodium and nedocromil sodium, w…
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- Safety and efficacy of lodoxamide in vernal keratoconjunctivitis. [Journal Article]
- CONCLUSIONS: Topical lodoxamide eye drops, when used for treatment of VKC, are effective with fewer adverse effects.
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- Eosinophils express muscarinic receptors and corticotropin-releasing factor to disrupt the mucosal barrier in ulcerative colitis. [Journal Article]
- CONCLUSIONS: We identified a neuroimmune intercellular circuit (from cholinergic nerves, via eosinophils to mast cells) that mediates colonic mucosal barrier dysfunction in patients with UC. This circuit might exacerbate mucosal inflammation.
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- Immediate hypersensitivity elicits renin release from cardiac mast cells. [Journal Article]
- CONCLUSIONS: Our findings disclose that immediate-type hypersensitivity elicits renin release from mast cells, activating a local renin-angiotensin system, thereby promoting norepinephrine release. As renin is stored in human heart mast cells, allergic reactions could initiate renin release, leading to local angiotensin formation and hyperadrenergic dysfunction.
- Optimal use of topical agents for allergic conjunctivitis. [Journal Article]
- In recent years, there has been renewed interest in the topical treatment of allergic conjunctivitis, a disorder that is involved in the common red-eye syndrome. Topical treatment for rapid relief of symptoms is most often preferred by the patient, although physicians are more cautious with the choice of an agent that might worsen symptoms due to contact irritation induced by the substance or its…
- Corticotropin-releasing hormone (CRH) regulates macromolecular permeability via mast cells in normal human colonic biopsies in vitro. [Journal Article]
- CONCLUSIONS: Our results suggest that CRH mediates transcellular uptake of HRP in human colonic mucosa via CRH receptor subtypes R1 and R2 on subepithelial mast cells. CRH-induced macromolecular uptake in human colon mucosa may have implications for stress-related intestinal disorders.
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- Secondary bacterial keratitis associated with shield ulcer caused by vernal conjunctivitis. [Case Reports]
- CONCLUSIONS: Bacterial keratitis associated with shield ulcer may be rarely observed in patients with vernal keratoconjunctivitis. Prompt diagnosis and treatment may prevent permanent complications and vision loss.
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- A clinicopathological analysis of the efficacy of lodoxamide 0.1% eye drops on the conjunctiva of patients with vernal keratoconjunctivitis seen at Guinness Eye Centre, Lagos University Teaching Hospital. [Journal Article]Niger Postgrad Med J. 2006 Mar; 13(1):35-40.NP
- CONCLUSIONS: Lodoxamide 0.1 ophthalmic solution is highly effective in alleviating the clinical signs and symptoms of Vernal Keratoconjunctivitis and its antiallergic activity is exerted by inhibiting migration of inflammatory cells mainly eosinophlis.
- Cardiac mast cell-derived renin promotes local angiotensin formation, norepinephrine release, and arrhythmias in ischemia/reperfusion. [Journal Article]
- Having identified renin in cardiac mast cells, we assessed whether its release leads to cardiac dysfunction. In Langendorff-perfused guinea pig hearts, mast cell degranulation with compound 48/80 released Ang I-forming activity. This activity was blocked by the selective renin inhibitor BILA2157, indicating that renin was responsible for Ang I formation. Local generation of cardiac Ang II from ma…
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- Efficacy and tolerability of newer antihistamines in the treatment of allergic conjunctivitis. [Review]
- Treatment for allergic conjunctivitis has markedly expanded in recent years, providing opportunities for more focused therapy, but often leaving both physicians and patients confused over the variety of options. As monotherapy, oral antihistamines are an excellent choice when attempting to control multiple early-phase, and some late-phase, allergic symptoms in the eyes, nose and pharynx. Unfortun…
- Topical treatments for seasonal allergic conjunctivitis: systematic review and meta-analysis of efficacy and effectiveness. [Review]
- CONCLUSIONS: Overall, these findings confirm the benefit of topical mast cell stabilisers and antihistamines over placebo for the treatment of allergic conjunctivitis. There is, however, insufficient evidence to recommend the use of one type of medication over another. Treatment preferences should therefore be based on convenience of use (with reduced frequency of instillation for some preparations), patient preference, and costs, especially as important side effects were not reported with any medication.
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- Seasonal allergic conjunctivitis. [Journal Article]
- Seasonal allergic conjunctivitis is rarely associated with permanent vision impairment; however, it is a relatively common condition that may compromise the quality of life of patients with this diagnosis. In extreme cases daily activities, including work, may be compromised. Numerous treatment options have become available for the relief of acute symptoms. Corticosteroids may be used for severe …
- Ocular allergic disease. [Journal Article]
- Ocular allergy is a common condition that usually affects the conjunctiva of the eye and is therefore often referred to as allergic conjunctivitis. The severity of the disease can range from mild itching and redness, as seen in seasonal allergic conjunctivitis, to the more serious vision threatening forms of ocular allergy which affect the cornea, such as atopic keratoconjunctivitis. The pathogen…
- Tear and serum eosinophil cationic protein levels in seasonal allergic conjunctivitis. [Journal Article]
- CONCLUSIONS: Increased serum and tear ECP levels in patients with SAC confirms that both local and systemic eosinophil activation occurs in SAC. However, clinical signs and symptoms of SAC were not found to be correlated with the degree of eosinophilic activity. Thus ECP does not seem to have an important role in clinical manifestations of SAC.
- Vernal keratoconjunctivitis in Thailand. [Randomized Controlled Trial]
- A prospective, cross-sectional and randomized cross-over study was conducted to study the clinical features and treatment outcome among Thai patients with vernal keratoconjunctivitis (VKC). History-taking and eye examinations were performed. Mild cases of VKC were given topical antihistamine four times daily. Moderate and severe cases of VKC were treated with topical lodoxamide four times a day. …
- [In vitro effects of antiallergic eyedrops on complement activation induced by particulate matter]. [Journal Article]
- CONCLUSIONS: Among the antiallergic eyedrops tested in this study, only Naabak and Tilavist were found to significantly inhibit complement activation triggered by particulate matters or pollen allergenic extract. Such an anticomplement activity confers these two molecules a potential in the therapeutic management of pollution-related pseudoallergic conjunctivitis.
- Effects of ketotifen 0.025% and lodoxamide 0.1% on eosinophil infiltration into the guinea pig conjunctiva in a model of allergic conjunctivitis. [Journal Article]
- The effects of ketotifen and lodoxamide on eosinophil infiltration were assessed in a guinea pig model of allergic conjunctivitis. The two active treatments were coded in this masked study in which 30 male guinea pigs, sensitized to chicken egg albumin (ovalbumin), were randomly assigned to one of three groups: Group 1, instillation of 0.9% NaCl into the conjunctival sac of both eyes; Group 2, in…
- [The state-of-the art and prospects for the pharmacological therapy of infectious and allergic eye diseases]. [Review]Vestn Ross Akad Med Nauk. 2003VR
- The inflammatory, infectious and allergic diseases of the eye still remain an acute problem in practical ophthalmology due to their high prevalence, relapsing clinical course, a growing frequency rate of mycotic and acanthoamebic keratitis and a growing number of resistant causative agents of bacterial keratitis. 55.3% of corneal pathologies are related with the herpes simplex virus, 37.3%--with …
- [Evaluation of the efficacy and safety of lodoxamide in patients with allergic eye diseases]. [Clinical Trial]Acta Med Croatica. 2002; 56(3):93-8.AM
- CONCLUSIONS: Lodoxamide was effective in reduction of symptoms and clinical signs of the ocular allergies. The best results were obtained if the drug was administered as a prophylaxis or very early in the course of the disease.
- Comparison of antiallergic drugs in an experimental model of ocular anaphylaxis. [Journal Article]
- CONCLUSIONS: Levacobastine and lodoxamide but none of the three other drugs mentioned above were found to be effective in decreasing vascular permeability.