Injection of Met-enkephalin, either subcutaneously (10 or 100 μg, s.c.), intracerebroventricularly (100 ng or 1 μg, i.c.v.) or into the mesencephalic central gray (100 ng), had no inhibitory effect on sexual behavior in female rats. If combined with [(R)-3-(N-hydroxy)-carboxamido-2-benzylpropa...

Despite the mesocorticolimbic dopaminergic pathway being one of the main substrates underlying stimulating and reinforcing effects induced by psychostimulant drugs, there is little information regarding its role in their effects at the immune level. We have previously demonstrated that acute exp...

Met-enkephalin (Tyr-Gly-Gly-Phe-Met) and its more stable analogs, Tyr-D-Ala-Gly-MePhe-Met-NHC3H7-iso (1) and Tyr-D-Ala-Gly-MePhe-Gly-NHC3H7-iso (2) significantly enhanced human T-cell proliferation in vitro after 5 days of incubation in the absence of mitogen. The activity was completely inhibit...

The effects of Met-enkephalin on the spontaneous and electrically evoked activity were investigated in longitudinal and circular strips isolated from different regions of the large intestine, i.e., proximal colon, distal colon and rectum. Met-enkephalin induced dose-dependent contractile respons...

This study used a rat model of Fetal Alcohol Syndrome to investigate whether combined prenatal and postnatal ethanol exposure affects met-enkephalin levels in the brains of male and female Long–Evans adult rats. Intragastric ethanol was administered to a group of rats (ET) from gestational day ...

Kyotorphin is a unique biologically active neuropeptide (l-tyrosine-l-arginine), which is reported to have opioid-like analgesic actions through a release of Met-enkephalin from the brain slices. N-methyl-l-tyrosine-l-arginine (NMYR), an enzymatically stable mimetic of kyotorphin, successfully c...

Methionine enkephalin ([Met5]-enkephalin, Opioid growth factor (OGF)) is a small neuropeptide with growth-related as well as immunomodulatory properties. OGF is distributed widely throughout the body, is both autocrine and paracrine produced, and has a very short half-life in serum. In addition ...

BackgroundInflammatory bowel diseases (IBD) are a group of chronic and recurrent gastrointestinal disorders that are difficult to control. Recently, a new IBD therapy based on the targeting of the endogenous opioid system has been proposed. Consequently, due to the fact that endogenous enkephali...

A novel immobilized nitrilase (I-N-l-D155) immobilized with D155 resin modified by l-lysine (L-D155) was synthesized and used in the production of (R)-(−)-mandelic acid ((R)-(−)-MA). FTIR spectra indicated that nitrilase has been introduced into L-D155 resin and the Schiff base was formed. The c...

A new rapid, simple, sensitive and high performance thin layer chromatography (HPTLC) has been established for the simultaneous determination of ascorbic acid and gallic acid in the freeze-dried pomegranate fruit juice and herbal formulation. HPTLC method was carried out using ethyl acetate: ace...

The objective of this study was to develop straightforward processes that could be applied to the large-scale production of β-cryptoxanthin in an attempt to facilitate investigation of its biological activity. An oleoresin obtained from crude extracts of marigold flowers (Tagetes erecta) with a...

A series of novel xanthine derivatives 2a-l incorporating benzoic acid moieties were rapidly generated by using strategy of scaffold-hopping from our previously reported scaffold uracil to xanthine, a scaffold of approved drug linagliptin. After systematic structure-activity relationship (SAR) s...

We have developed a series of adamantane carboxylic acid derivatives exhibiting potent diacylglycerol acyltransferase 1 (DGAT1) inhibitory activities. Optimization of the series led to the discovery of E-adamantane carboxylic acid compound 43c, which showed excellent in vitro activity with an IC...

A new class of quinoline derivatives, bearing amino chains at C-4 and a styryl group at C-2, were tested on Leishmania donovani promastigotes and axenic and intracellular Leishmania pifanoi amastigotes. The introduction of the C-4 substituent improves the activity, which is due to interference w...

Bridging two molecules of an organic thiol with the 3,5-dimethylenebenzoic acid (Dmb) group produces a rigid five-carbon Dmb crosslink that is stable to disulfide reducing agents. Radical bromination of 3,5-dimethylbenzoic acid or its succinimido ester gave four α-brominated products. So NMR-pu...

The correct application of bio(iso)steric replacement, a potent tool for the design of optimized compounds, requires the continuous development of new isosters able to respond to specific target requirements. Among carboxylic acid isosters, as the hydroxylated pentatomic heterocyclic systems, th...

The pharmacokinetics of the antitoxic and anticarcinogenic compounds diethyldithiocarbamate, prolinedithiocarbamate and sarcosinedithiocarbamate were compared in rats. The bioavailability, the distribution in the organism, the oxidation to thiuramdisulfides, the cleavage to CS2 and the excretion...

The effect of collagen peptides (CPs) administration in early basic enteral nutrition (EN) intervention after burn injury on intestinal barrier function was investigated in mice model. Burn-induced increases of intestinal permeability and disruption of intestinal barrier integrity were significa...

Aim To compare the efficacy of a new application form of hydrocortisone 17-butyrate (H17-B), 0.1% topical emulsion (Locoid Crelo®) with that of betamethasone 17-valerate (BMV) 0.1% scalp lotion (Betnovate® lotion).Methods Erythema, induration, scaling, pruritus and overall severity of the diseas...

A series of pyrido[3′,2′:4,5]furo[3,2-d]pyrimidines (PFP) were synthesized and tested for phosphodiesterase type 4 (PDE4) inhibitory activity, with the potential to treat asthma and chronic obstructive pulmonary disease (COPD). Structure–activity relationships within this series, leading to a...