Development of novel indole-linked pyrazoles as anticonvulsant agents: A molecular hybridization approach.

A series of 3-{2-[1-acetyl-5-(substitutedphenyl)-4,5-dihydropyrazol-3-yl]hydrazinylidene}-1,3-dihydro-2H-indol-2-ones 24-43 was synthesized using an appropriate synthetic route and evaluated experimentally by the maximal electroshock test. These compounds were evaluated for antidepressant and antianxiety activities. The most active compound, 3-{2-[1-acetyl-5-(4-chlorophenyl)-4,5-dihydropyrazol-3-yl]hydrazinylidene}-1,3-dihydro-2H-indol-2-one 25, exhibited an ED of 13.

Development of lamivudine liposomes by three-level factorial design approach for optimum entrapment and enhancing tissue targeting.

This work aimed to encapsulate lamivudine in liposomes for targeted delivery to HIV reservoirs and thereby reduce its side effects. The lamivudine liposomes were prepared by thin film hydration method using 3 factorial design and characterised for vesicle size, % drug entrapment efficiency, polydispersity index etc. Optimisation by graphical and numerical methods was carried out by fixing minimum and maximum limits for each response.

Formulation and statistical optimization of self-microemulsifying drug delivery system of eprosartan mesylate for improvement of oral bioavailability.

The present investigation is aimed to design a statistically optimized self-microemulsifying drug delivery system (SMEDDS) of eprosartan mesylate (EM). Preliminary screening was carried out to find a suitable combination of various excipients for the formulation. A 3(2) full factorial design was employed to determine the effect of various independent variables on dependent (response) variables.

Gonadotropin-releasing hormone agonist prevents l-arginine induced immune dysfunction independent of gonadal steroids: Relates with a decline in elevated thymus and brain nitric oxide levels.

The present study was carried out to find out the effect of leuprolide, a gonadotropin-releasing hormone (GnRH) receptor agonist, on l-arginine induced immunosuppression, and relates with brain and thymus levels of nitric oxide (NO). Further, the effect of leuprolide was studied in sham operated, ovariectomized and castrated mice to understand the role of sex steroids in l-arginine induced immunosuppression. Treatment with l-arginine (250, 500, 1000 mg/kg/i.

Formulation of Thermosensitive in situ Otic Gel for Topical Management of Otitis Media.

Antibiotics and antiinflammatory agents are the primary and main therapeutic categories in the treatment of otitis media. One of the simpler and feasible approaches of minimizing the problem of repeated use and subsequent resistance is development of sustained release formulation. Therefore, the present investigation aimed to develop a sustained release in situ gel formulation containing combination of broad spectrum antibiotic and antiinflammatory agents for the management of otits media.

Immunohistochemical evidence for the involvement of gonadotropin releasing hormone in neuroleptic and cataleptic effects of haloperidol in mice.

Blockade of dopamine D2 receptor by haloperidol is attributed for neuroleptic and cataleptic effects; and also for the release of gonadotropin releasing hormone (GnRH) from the hypothalamus. GnRH agonist is reported to exhibit similar behavioural effects as that of haloperidol, and pre-treatment with GnRH antagonist is shown to attenuate the effects of haloperidol, suggesting a possibility that GnRH might mediate the effects of haloperidol. To substantiate such possibility, the influence of haloperidol on GnRH immunoreactivity (GnRH-ir) in the brain was studied in vehicle/antide pre-treated mice by peroxidase-antiperoxidase method.

A possible role of endogenous central corticotrophin releasing factor in lipopolysaccharide induced thymic involution and cell apoptosis: effect of peripheral injection of corticotrophin releasing factor.

The aim of the study was to investigate the role of endogenous peripheral and central corticotrophin-releasing factor (CRF) following lipopolysaccharide (LPS) challenge on thymic involution and apoptosis. Administration of LPS (100 μg/mouse, ip) led to thymic involution, to a decrease of CD4+CD8+ thymocyte subset, and to fragmentation of thymic DNA. Pretreatment of LPS challenged mice with intracerebroventricular α-helical CRF (a CRF antagonist) attenuated the effect of LPS however, intraventricular administered α-helical CRF failed to affect LPS response on thymus.

Gonadotropin-releasing hormone agonist selectively augments thymopoiesis and prevents cell apoptosis in LPS induced thymic atrophy model independent of gonadal steroids.

Lipopolysaccharide (LPS) causes acute thymic atrophy, a phenomenon that has been linked to immune dysfunction and poor survival during sepsis. The systemic response to LPS involves a rise in glucocorticoids and proinflammatory cytokines which contribute greatly to thymic involution and apoptosis. Gonadotropin-releasing hormone (GnRH) analog exerts thymopoietic regulatory effects and possesses immunostimulant properties.