The activity of three angiotensin I converting enzyme (ACE) inhibitors with unique related structures was assessed in vitro and in vivo. The three compounds were (S)(-)-1,2,3,4-tetrahydro-2- (3-mercapto-1-oxopropyl)-3- isoquinolinecarboxylic acid (EU-4865), 1,2,3,4-tetrahydro-2-(3-mercapto-1-oxo...

Fatty acid binding protein 4 (FABP4) is a potential drug target for diabetes and atherosclerosis. For discovering new chemical entities as FABP4 inhibitors, structure-based virtual screening (VS) was performed, bioassay demonstrated that 16 of 251 tested compounds are FABP4 inhibitors, among whi...

Efficient SO3H-functionalized metal organic framework, UiO-66-NH-SO3H, has been successfully prepared through a post-synthetic modification strategy of UiO-66-NH2 with Chlorosulfonic acid reagent. The UiO-66-NH2 has been synthesized by an ultrasound-assisted (US) method and compared with the con...

The design, synthesis and biological evaluation of a library of 1,2,3-triazole carboxylates incorporating carboxylic acid, hydroxymethyl, carboxylic acid hydrazide, carboxamide and benzenesulfonamide moieties is disclosed. All the novel compounds were investigated for their inhibition potential ...

PurposeTamsulosin is associated with intraoperative floppy iris syndrome (IFIS), an important risk factor for complications during cataract surgery. Significant efforts have been made to increase awareness of the risks associated with tamsulosin, and educational initiatives have fostered the upt...

BackgroundTamsulosin, an α1A-adrenergic receptor inhibitor, is prescribed to treat benign prostatic hyperplasia in men >60 years of age, the same demographic most susceptible to abdominal aortic aneurysm. The goal of this study was to investigate the effect of tamsulosin on abdominal aortic ane...

BackgroundPostoperative urinary retention (POUR) is common. Selective alpha-1 adrenergic antagonists, such as tamsulosin, are effective for treating urinary retention. The purpose of this study is to determine whether perioperative prophylactic tamsulosin reduces the incidence of POUR following ...

PurposeFluorinated and non-fluorinated valproic acid (VPA) analogues with hydroxamic acid moieties were tested for their teratogenic, anticonvulsant and neurotoxic potencies in mice.

3,6-Dichloro-[1,2,4,5]tetrazine has been found to act as an efficient azadiene equivalent in inverse electron demand [4+2] cyclisations with a range of alkenes and alkynes, allowing rapid access to a range of highly functionalised pyridazines.

A synthetic gene for the hydra neuropeptide head activator (HA) was used to produce large amounts of an HA bacterial fusion protein. From this protein an HA-containing fragment was cleaved out, attached in high copy number to carrier proteins, and used as an immunogen to produce monoclonal antib...

A highly sensitive and specific radioimmunoassay for the head activator has been developed which utilises tritriated head activator. The assay is sensitive in the range of 40–200 fmol. Immunochemical studies showed that the antiserum recognised the intact molecule better than any of the fragmen...

The present study aimed to investigate the effects of single or continuous administration of a neurokinin 3 receptor agonist, senktide, on hormonal and follicular dynamics in follicular phase goats. Goats were injected with PGF2α in the luteal phase and treated with an intravaginal progesterone...

SummarySirtuins are protein deacetylases regulating aging processes and various physiological functions. Resveratrol, a polyphenol found in red wine, activates human Sirt1 and inhibits Sirt3, and it can mimic calorie restriction effects, such as lifespan extension in lower organisms. The mechani...

No-carrier-added (NCA) R(+)-7-chloro-8-hydroxy-3-(3′-[18F]fluoropropyl)-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine (2b) (an analog of dopamine D-1 receptor ligand SCH 23390), ethyl 8-fluoro-5,6-dihydro-5-(3′-fluoropropyl)-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate (4b) and 3′-[18...

Four nitro- and fluorobenzamides (1–4) have been synthesized in good yields from nitro- and fluoro-substituted benzoyl chloride with 4-amino-1-benzylpiperidine. In vitro studies showed that these compounds have high affinities to σ receptors. N-(N-Benzylpiperidin-4-yl)-2-fluorobenzamide (3), i...

Introduction2-[18F]Fluoroethoxy and 3-[18F]fluoropropoxy groups are common moieties in the structures of radiotracers used with positron emission tomography. The objectives of this study were (1) to develop an efficient one-step method for the preparation of 2-[18F]fluoroethanol (2-[18F]FEtOH) a...

There is great interest in the application of positron labeled ligands to map the dopamine receptor in vivo. A series of fluorine-18-labeled N-alkyl and N-fluoroalkyl spiroperidol (SP) derivatives N-methyl[18F]SP; N-ethyl[18F]SP; N-(2-[18F]fluoroethyl)SP; N-propyl[18F]SP; N-(3-[18F]fluoropropyl)...

N-(3-Fluoropropyl)-N-norbuprenorphine (3a) and N-(3-fluoropropyl)-N-nordiprenorphine (4a) were synthesized by N-alkylation of norbuprenorphine (1) and nordiprenorphine (2) with 1-bromo-3-fluoropropane. The corresponding no-carrier-added (NCA) N-(3-[18F]fluoropropyl)-N-norbuprenorphine (3b) and N...

The neuroleptics haloperidol and spiperone potentiated anti-μ induced murine B-lymphocyte proliferation in vitro and lowered the threshold of anti-μ antibody needed to trigger proliferation. Because haloperidol and spiperone are best known for actions at D2, 5HT2, α1 and sigma (σ) receptors,...

The development of a high affinity dopamine receptor ligand labeled with the positron emitting radionuclide, 18F (t12 = 110 min), is of considerable interest for imaging and quantification of dopamine receptors in vivo. Derivatives of spiperone, a dopamine antagonist, labeled with 18F have been ...