Background & Aims: The aim of this study was to evaluate the dose-ranging pharmacodynamic effects of renzapride, a 5-hydroxytryptamine 4 (5-HT4) receptor full agonist/5-HT3 receptor antagonist, on gastrointestinal transit and symptoms in patients with constipation-predominant irritable bowel syn...

N-[1-(2-Benzo[b]thiophenyl)cyclohexyl]piperidine (BTCP)-related molecules were prepared by means of chemical modulation of the 3 rings which constitute this dopamine (DA) and norepinephrine (NE) uptake inhibitor. Tested in vitro (binding to the DA uptake complex and to the PCP receptor sites, in...

Summary3-Methylpiperidine derivatives of 1-[1-(2-thienyl)cyclohexyl]piperidine (TCP) and l-[1-(2-benzo[b]thiophenyl)cyclohexyl] piperidine (BTCP) were obtained in their racemic and homochiral forms. They have been tested for their affinity for the PCP receptor labeled with [3H]TCP and for the do...

Congeners of the potent dopamine (DA) re-uptake inhibitor 1-[1-(2-benzo[b]thiophenyl)cyclohexyl]piperidine (BTCP) are unexpectedly able to bind in the rat cerebellum, although this structure is devoid of dopaminergic nerve endings. In line with previous studies the hypothesis that they bind to l...

1-[1-(2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) and cocaine bind to the neuronal dopamine transporter (DAT) to strongly inhibit dopamine (DA) reuptake. Although similar to acute administration, cocaine and BTCP produce sensitization and tolerance, respectively, on chronic ...

Combining the specificity of radioimmunoscintigraphy and the high sensitivity of PET in an in vivo detection technique could improve the quality of nuclear diagnostics. Positron-emitting nuclide 76Br (T1/2=16.2 h) might be a possible candidate for labeling monoclonal antibodies (mAbs) and their ...

N-succinimidyl-3-(tri-n-butylstannyl)benzoate (m-BuATE), N-succinimidyl-3-(tri-methylstannyl)benzoate (m-MeATE) and N-succinimidyl-4-(tri-n-butylstannyl)benzoate (p-BuATE) were synthesized and radioiodinated using either N-chlorosuccinimide (NCS) or t-butylhydroperoxide (TBHP) as the oxidant. Ra...

A method is described for labeling proteins with 7.2 h half-life 211At. The α particle-emitting nuclide was coupled to goat IgG using an N-succinimidyl 3-(tri-n-butylstannyl) benzoate intermediate. The reaction and purification sequence requires about 2 h to produce 211At-labeled IgG in 25–40%...

N-Succinimidyl 4-methyl-3-(tri-n-butylstannyl)benzoate (MATE) was synthesized in two steps from 4-methyl-3-iodobenzoic acid. Radioiododestannylation of MATE proceeded more slowly than N-succinimidyl 3-(tri-n-butylstannyl)benzoate (ATE), but for reaction periods of 10 min or more, identical yield...

N-Methyl-N-2-oxopropylnitrosamine (MOP) induces pancreatic tumors in hamsters. As models for the putative proximate carcinogenic α-hydroxy derivatives, we studied N-acetoxymethyl-N-2-oxopropylnitrosamine (AMOP) and N-methyl-N-(1-acetoxy-2-oxopropyl)nitrosamine (MAOP). AMOP was synthesized from ...

Volatile N-nitrosamines have been found in rubber products including gloves, balloons, toys, baby bottle teats, soothers, and condoms. N-Nitrosamines are potent carcinogens, and therefore, European legislation has limited the release of N-nitrosamines and N-nitrosatable compounds in teats and so...

The reversible oxidation of protein cysteine residues (Cys-SH) is a key reaction in cellular redox signaling involving initial formation of sulfenic acids (Cys-SOH), which are commonly detected using selective dimedone-based probes. Here, we report that significant portions of dimedone-tagged pr...

A novel carbon paste sensor based on carbon nanotubes (CNTs) was successfully developed for the sensitive and selective determination of bambuterol hydrochloride (BAM). The sensor is based on bambuterol-tetraphenyl borate (BAM-TPB) as a recognition ion-pair, dibutyl phthalate (DBP) as plasticize...

The adjuvanticity of sodium houttuyfonate (SH) and its mechanism were studied in this research. Significant enhancement of antibody production was observed when co-injected with antigen. The levels of anti-BSA antibodies were measured by enzyme-linked immunosorbent assay (ELISA). The possible me...

ObjectiveTo study antimicrobial effect of Sodium houttuyfonate (SH) on Staphylococcus epidermidis (SE) and Candida albicans (CA).

In this report, 120 healthy one-day-old AA broilers were divided into six groups. Groups 1–4 received 100, 200, 400 and 800 mg/L of sodium new houttuyfonate (SNH) with IB vaccine H120 respectively. Group 5 received PBS and H120 and group 6 IL-2 and H120. The chickens were inoculated at 7 and 14...

Summary[(Nα-Me)Leu7]LRF, (pGlu-His-Trp-Ser-Tyr-Gly-(Nα-Me)Leu-Arg-Pro-Gly-NH2), and [D-Ala6,(Na-Me)Leu7]LRF, (pGlu-His-Trp-Ser-Tyr-D-Ala-(Nα-Me) Leu-Arg-Pro-Gly-NH2), were synthesized by solid-phase methodology. The peptides were assayed by the in vitro system against LRF and found to have ca...

(−)-(1S,2R,3R,4S)-1,2-Epoxy-1-methyl-4-(1-methylethyl)-cyclohex-3-yl acetate has previously been identified as the active compound of Minthostachys tomentosa responsible for the insecticidal activity against Oncopeltus fasciatus. Its structure was initially assigned on the basis of spectral data...

A series of esters of 4-acetyl, 4-trifluoroacetyl- and 4-(3-chloropropionyl)aminobenzenethiosulfoacids (twenty-four compounds) were synthesized and characterized by elemental analysis, 1H NMR and IR spectroscopy. The antibacterial activity of the novel candidates has been screened using the agar...

We examined the in vivo mutagenicity of 2-[2-(acetylamino)-4-[bis(2-hydroxyethyl)amino]-5-methoxyphenyl]-5-amino-7-bromo-4-chloro-2H-benzotriazole (PBTA-6) and benzo[a]pyrene (BaP) by using transgenic (Tg) zebrafish carrying the mutational target gene rpsL. PBTA-6 is one of the PBTA-type compoun...