1. The mechanism of gastric mucosal protection by an antiulcer agent, nitecapone, against injury was investigated in rats with and without indomethacin pretreatment.2. Animals received intragastrically either a dose of nitecapone or vehicle alone, followed by ethanol given at various intervals u...

Background. Nitecapone has been shown to have a protective effect against ischemia-reperfusion injury in experimental heart transplantation and in Langendorff preparations. This prospective, randomized study assessed the effects of nitecapone in patients who had coronary artery bypass grafting.M...

1.1. The effect of a new antiulcer agent, nitecapone, on the synthesis and secretion of sulfomucin in gastric mucosa was investigated using mucosal segments incubated in the presence of [3H]proline, [3H]glucosamine and [35S]sulfate.2.2. The drug, while showing no discernible effect on the apomuc...

The antioxidant properties of nitecapone, a catechol derivative and an inhibitor of catechol-O-methyltransferase, were reported recently. In the present study, the influence of nitecapone on isolated rat heart ischemia-reperfusion injury was investigated to elucidate its cardioprotective role. N...

Nitecapone [3-(3,4-dihydroxy-5-nitrophenyl)methylene-2,4-pentanedione] [OR-462] is a catechol-O-methyltransferase inhibitor with gastroprotective properties. Recently, its antioxidant properties have been discovered: It scavenges peroxyl radicals (ROO.) and thus spares glutathione. Further exami...

Neuropathic pain is caused by damage or malfunctioning of the nervous system. It is fairly common and more resistant to treatment than other types of pain. Since nitecapone, an inhibitor of catechol-O-methyl-transferase (COMT), has decreased neuropathic symptoms in diabetic rats, we studied its ...

We have investigated whether any of the three isoforms of endothelin (ET) ET-1, ET-2 and ET-3 or the structurally similar peptide sarafotoxin S6b is mitogenic on its own for rat vascular smooth muscle cells in culture. DNA synthesis was determined by a peroxidase-linked double antibody technique...

Endothelin-1 (ET-1), endothelin-3 (ET-3) and sarafotoxin S6b (SRFTX) produced a concentration-dependent contraction of the guinea-pig isolated bronchus. In untreated preparations, SRFTX was about 10 times more potent than ET-1 or ET-3 and produced a greater maximal effect. Mechanical removal of ...

The three chimera peptides of sarafotoxins S6b (SRTb) and S6c (SRTc), [Thr2SRTb, [Asn4]SRTb and [Glu9]SRTb, were synthesized chemically. From the comparisons of lethality, vasoconstrictor activity and receptor binding activity of SRTb, SRTa ([Asn13]SRTb), SRTc ([Thr2Asn4Glu9Asn13]SRTb), [Thr2SRT...

Snake venom-derived sarafotoxin S6B (SRT) and porcine endothelium-derived endothelin-1 (ET) have striking structural similarities. In conscious, freely-moving rats, ET (0.67 nmol/kg) produced a transient tachycardia and fall in arterial blood pressure which was followed by a long-lasting increas...

Conscious, Long-Evans rats, chronically-instrumented for the direct measurement of intra-arterial and central venous pressures and ascending aortic blood flow (i.e. cardiac output), were given bolus, intravenous doses (4 and 40 pmol) of endothelin-1, -2, or -3 or sarafotoxin S6b in random order....

Sarafotoxin S6b (STX-b), a peptide toxin isolated from the venom of the Israeli burrowing asp, Atractaspis engaddensis, consists of 21 amino acid residues with four cysteines at positions 1,3,11 and 15. In the present study, we compared the cardiovascular effects of two synthetic STX-b analogues...

Sarafotoxin-S6b has been synthesized and studied by 1H NMR in 5050 acetonitrile/water mixture. All spin systems were identified and assigned with the aid of 2D experiments. On the basis of these data, a 3D structure of sarafotoxin is proposed and compared to that of [Nle7]endothelin obtained in ...

Endothelins (ETs) and sarafotoxin-S6b belong to a family of extremely potent vasoconstrictors which may also have a role as neuropeptides or neuromodulators in the central nervous system (CNS). We show, using single cell dynamic video imaging of intracellular free calcium ions ([Ca2+]i), that bi...

In the isolated perfused mesenteric vascular bed, porcine endothelin (ET) and sarafotoxin S6b produced direct vasoconstriction and potentiated nerve stimulation-induced vasoconstriction. ET also enhanced the vasoconstrictor response to exogenous norepinephrine (NE). Basal or stimulated endogenou...

The receptors mediating smooth muscle response to endothelin-1 and sarafotoxin S6b in the human umbilical artery were investigated in vitro. Both agonists induced contractions that were unaffected by the endothelin ETB receptor antagonist BQ 788 (10−9, 10−8, 10−7 M). The non-selective endothelin...

As an extension of our project aimed at the search for new chemotherapeutic agents against Chagas disease and toxoplasmosis, several 1,1-bisphosphonates were designed, synthesized and biologically evaluated against Trypanosoma cruzi and Toxoplasma gondii, the etiologic agents of these diseases, ...

A new glycosyl acceptor to be used in sialylation was designed as a 3-hydroxy derivative of 4-methoxyphenyl β-d-galactopyranoside with 2-O-acetyl group and O-4 and O-6 protected as benzylidene acetal. Two alternative syntheses of this compound were compared. Sialylation of 3-OH group of the gly...

Oligonucleotide-templated Ag nanoclusters (DNA–Ag NCs) prepared from AgNO3 using an oligonucleotide (5′-TAACCCCTAACCCCT-3′) as a template and NaBH4 as a reducing agent have been used for sensing of adenosine 5′-triphosphate (ATP). The fluorescence intensity and emission wavelength of DNA–Ag...

This work designs a new label-free aptasensor for the colorimetric determination of small molecules (adenosine 5′-triphosphate, ATP) by using visible gold nanoparticles as the signal-generation tags, based on target-triggered hybridization chain reaction (HCR) between two hairpin DNA probes. Th...