Antagonists of type 1 cannabinoid receptors (CB1) may be useful in treating diabetes, hepatic disorders, and fibrosis. Otenabant (1) is a potent and selective CB1 inverse agonist that was under investigation as an anti-obesity agent, but its development was halted once adverse effects associated...

The estrogenicity and antiestrogenlcity of the biologically active metabolite of the contraceptive anordrin was investigated for its actions on both the uterus and ovary. Anordiol (30 μg), administered s.c. to ovariectomized mice did not significantly increase wet weight, soluble protein conten...

We describe the chemical synthesis of the 2β-propionate-17β-hemisuccinate and 2β-hemisuccinate-17β-propionate diesters of anordiol (2α,17α-diethynyl-A-nor-5α-androstane-2β,17β-diol) and the method for coupling them to bovine serum albumin and Affi-gel 102, in order to prepare antibodies...

Anordiol (2α,17α-diethynyl-A-nor-5α-androstane-2β,17β-diol) has been variously characterized as an estrogen and as an antiestrogen. To more completely understand the pharmacological properties of this contraceptive steroid, simultaneous responses were studied in uterine, vaginal, and hepati...

In view of the unexpected ability of anordrin to synergize with RU 486 in terminating pregnancy, it was pertinent to examine the actions of the dihydroxylated metabolite of anordrin, anordiol, alone and in combination with RU 486. Doses of RU 486 (1 mg/kg/day) and anordiol (0.6 mg/kg/day) that w...

RU486, an antiprogestational agent, and anordiol (dihydroxylated metabolite of anordrin) which has an estrogenic and antiestrogenic activity, are known to inhibit fertility. These agents were administered orally, alone or together, to rats prior to implantation, on Day 2 of pregnancy. Control an...

The effectiveness of mifepristone, onapristone, and ORG 31806 alone or in combination with anordiol to terminate pregnancy in the rat was evaluated. ORG 31806 at a dose of 2 mg/kg/day, mifepristone at 4 mg/kg/day, and onapristone at 8 mg/kg/day, terminated pregnancy in all treated animals. Anord...

Anordiol, the dihydroxylated metabolite of anordrin, is an antiestrogen with estrogenic activity that is known to inhibit fertility. The following study was conducted to determine the mechanism of this antifertility effect. Anordiol was administered orally to rats, prior to implantation, on Day ...

This work concerns the interaction of prenoxine sodium (PRX) and bovine serum albumin (BSA), which was conducted by spectroscopic means: fluorescence spectra, ultraviolet–visible spectra (UV–vis) and circular dichroism spectra (CD spectra) in physiological conditions. The results revealed the ...

The production of reactive oxygen species (ROS) associated with excimer laser irradiation is recognized as a possible cause of corneal haze following photorefractive keratectomy (PRK). Our work was aimed at investigating in vitro the oxidative effects induced by subablative laser fluences and at...

A simple, economical, and green approach to the synthesis of 5,5′-((2,4-dichlorophenyl)methylene)bis(1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione) 4 using a tandem Aldol condensation-Michael addition process in aqueous diethylamine medium was described. The 3D structure of the latter was confi...

Condensation reaction of 5-bromo-1H-indole-3-carbaldehyde and 1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione in ethanol under reflux conditions furnished the formation of 5-((5-bromo-1H-indol-3-yl)methylene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione indole in a very good yield. The desired co...

The newly Ni++-1,3,5-tribenzyl-1,3,5-triazine-2,4,6-(1H,3H, 5H)-trione coordinated polymeric MOFs were carefully synthesized via microwave-assisted hydrothermal technique. Theoretical investigations were predicted by two different stereo-orientations which can be present inside unite cell of Ni(...

BackgroundCough is a common presenting symptom in patients with idiopathic interstitial pneumonia (IIP); it is often disabling, and lacks effective treatment. Studies in animals suggest that carcainium chloride, a quaternary derivative of the local anesthetic lidocaine, is able to inhibit experi...

Publisher SummaryThis chapter discusses the analytical profile of nalorphine hydrobromide. Its generic names are allorphine, anarcon, antrophine, lethidrone, nalline, and norfin. It is an odorless, white to creamy white crystalline powder. Its melting range is about 260° with decomposition. It ...

Polystyrene resin was functionalized by diethanolamine for the efficient removal of p-toluenesulfonic acid (p-TSA) from aqueous solution. Functionalized adsorbent (DEA-PS) was characterized by elemental analysis, Fourier transform infrared spectroscopy, point of zero charge measurement and field...

The reaction of cyclic γ,δ-epoxy esters with p-toluenesulfonic acid monohydrate is described. The reaction carried out in benzene or methylene chloride gave tosyloxy lactones as product. The ethoxy or methoxy lactones were obtained when ethanol or methanol were used as solvent. A mechanism of ...

A new organic crystal, 2-amino 4, 6 dimethoxypyrimidine p-toluenesulfonic acid monohydrate (2ADPTS) was synthesized and crystals were grown from ethanolic solution by the slow evaporation method. Formation of the new crystalline compound was confirmed by a single crystal X-ray diffraction study....

The 1:1 p-toluenesulfonic acid–water complex, p-toluenesulfonic acid itself and the p-toluenesulfonate anion were studied at HF and B3LYP/6-31+G(d,p) levels of theory. Full geometry optimizations of the aforementioned species reveal non-existence of ionic minima on the explored 1:1 p-toluenesul...

Due to the increasing concerns about the availability and accessibility of fossil fuel reserves, and the subsequent effect of using them on climate change, production of green energy has recently become a hot area of interest in the research field. As a renewable energy source, biomass conversio...