SummaryFibroblast growth factor 21 (FGF21) is a metabolic hormone with pleiotropic effects on glucose and lipid metabolism and insulin sensitivity. However, the role of FGF21 in hypertension remains elusive. Here we show that FGF21 deficiency significantly exacerbates angiotensin II-induced hype...

ObjectivesThe authors sought to evaluate cardiac activity of angiotensin-converting enzyme (ACE) and ACE2 after heart transplantation (HT) and its relation with acute rejection (AR) and chronic allograft vasculopathy (CAV).

BackgroundNeprilysin inhibitors (NEPi) are assisting the renin-angiotensin system (RAS) inhibitors in halting diabetic cardiomyopathy (DCM). Away from conventional tactic, a recent report revealed the renoprotective potential of NEPi and angiotensin-converting enzyme (ACE2) activator combination...

Angiotensin converting enzyme 2 (ACE2) degrades vasoconstricting angiotensin II (Ang II) into angiotensin (1–7), exerting protective effects in cardiovascular system; thus, ACE2 is considered as a novel target for cardiovascular therapy. The objectives of this study were to identify ACE2 up-reg...

Viroids are plant infecting, non - coding RNA molecules of economic importance. Potato spindle tuber viroid (PSTVd), the type species of Pospiviroidae family, has been shown to be affected by specific RNA silencing pathways. Dicer like 1 (DCL1), a key player in micro RNA (miRNA) pathway has been...

In the early 1990’s, we reported on the low-molecular selective fXa inhibitor DX-9065a having two amidino groups. However, it had poor oral bioavailability due to its strong basic amidino groups. To obtain fXa inhibitors with improved oral bioavailability, we investigated various non-amidino fX...

From the structure activity relationship, two new analogs, 2 and 3, of the potent progesterone antagonist mifepristone 1 have been designed. The syntheses of these two analogs have been achieved in eleven steps through modified synthetic sequences and improved procedures starting from (+)-estron...

A series of 1-deoxy analogs of CP-47,497 (8 and 13, n = 0–7) and 1-deoxy analogs of CP-55,940 (9, n = 0–7) have been synthesized and their affinities for the cannabinoid CB1 and CB2 receptors have been determined. Although the majority of these compounds exhibit selectivity for the CB2 recepto...

Three 1-methoxy analogs of CP-47,497 (7, 8, and 19) have been synthesized and their affinities for the cannabinoid CB1 and CB2 receptors have been determined. Although these compounds exhibit selectivity for the CB2 receptor none have significant affinity for either receptor. Modeling and recept...

Cannabicyclohexanol (CP-47,497-C8) is a representative of a group of cannabimimetic cyclohexylphenols which is added to herbal mixtures as a cannabis substitute since 2008. Although in the beginning CP-47,497-C8 was the main ingredient of “Spice” and similar products, it was partly replaced by...

Failures of self-regulation in problem and pathological gambling (PPG) are thought to emerge from failures of top-down control, reflected neurophysiologically in a reduced capacity of prefrontal cortex to influence activity within subcortical structures. In patients with addictions, these impair...

Tolcapone and entacapone are two potent catechol-O-methyltransferase (COMT) inhibitors with a similar skeleton and displaying similar pharmacological activities. However, entacapone is a very safe drug used widely in the treatment of Parkinson's disease, while tolcapone is only in limited u...

This work investigates the crystal quality of SiGe layers grown at low temperatures using trisilane, and germane precursors. The crystal quality sensitivity was monitored for hydrogen chloride and/or minor oxygen amount during SiGe epitaxy or at the interface of SiGe/Si layers. The quality of th...

An efficient large-scale preparative synthesis of biologically interesting β,β,β-trifluoroalanine through the biomimetic transamination of the ethyl trifluoropyruvate has been developed. The azomethine—azomethine isomerization of the N-(1-phenyl)ethylimine of ethyl trifluoropyruvate to the N...

1. Pharmacological properties of KT2-230 (benzothiazepine derivative), a newly synthesized vasorelaxing agent, were studied.2. In the anesthetized dogs, KT2-230 increased the femoral and vertebral blood flow without effect on systemic blood pressure.3. In rabbit aorta, KT2-230, methysergide and ...

The 1,2-naphthoquinonediazide-(2)-6- and -7-sulfonic acid esters (7c, 7d) have been synthesized for first time starting from the 1-naphthyl-amine-6- and -7-sulfonic acids (1c, 1d), respectively, via Bucherer reaction, nitrosation, reduction, diazotation, sulfochlorination, esterification. The sy...

Different molecular environments were found for the two 1,2-naphthoquinone-2-diazide (NQD) substituents in 2,4-di-(1,2-naphthoquinone-2-diazide-5-sulphonyl-oxy)-benzophenone (2,4-NQD2-BP), detected by quantum chemical calculations of the molecular structure and by single-crystal X-ray analysis o...

The thermal reactions of o-naphthoquinone diazide (NQD) compounds as a material for photoresists were studied in comparison with their photochemical reactions. An NQD compound decomposed at around 140°C and further reacted in the presence of an alcohol in the solution to yield an indenecarboxyl...

Native hirudin is a heterogenous polypeptide obtained from the medicinal leech, Hirudo medicinalis. Recent advances in molecular biological techniques have led to the availability of large amounts of hirudin in the recombinant form. Recombinant hirudins (rH) are currently being investigated for ...

IntroductionThere are continuing needs for new antithrombotic agents and procedures. We hypothesized that the slowly cleared recombinant fusion proteins barbourin–albumin (BLAH6) and hirudin–albumin (HLAH6) would be effective in limiting fibrin(ogen) and/or platelet deposition in a rabbit mode...