Comparative biochemical and pharmacological investigations of various newly developed opioid receptor ligands

Bentley analogues: In vitro competition binding experiments all derivatives showed low subnanomolar affinity to MOR. For DOR the ligands showed comparable binding affinities than the selective DOR agonist Ile5,6-deltorphin II peptide ligand except 8 (Ki > 3000 nM). In the KOR binding assays the analogues still displayed nanomolar affinities. In G-protein activity measurements compound 1f, 2a, 2b had antagonistic; 1e, 2c, 8 had partial agonistic and 2d, 4, 5, 7 had full agonistic effects. Ligands were examined in G-protein activation tests in rat brain membranes, the selectivity could not be observed as the receptor selective antagonists such as Cyp, NTI, nor-BNI and the selective agonists such as DAMGO, Ile5,6-deltorphine II, U-69,593 are not able to inhibit the effects of the extremely potent Bentley analogues. In vivo tests in osteoarthritis inflammatory model the thevinol derivatives showed a significant antiallodynic effect, while orvinol derivatives, except for 2c, did not display this effect. Oligopeptides: In competition binding assays the KYNA‐containing peptide, KA1 bound selectively to the MOR with a low Ki value and a high selectivity ratio, the other oligopeptides also showed selectivity to MOR, except K3, which bound to MOR and DOR with similar affinity. In the G-protein activition tests the EM-2 containing compounds, K2 and K3 stimulated G-protein with low efficacy, compound KA1, K4, K5 behaved as full agonists, while K6 had efficacy and potency higher than those of the reference compound DAMGO. In functional binding assays all oligopetides were inhibited by Cyp (MOR) and NTI (DOR) in rat brain membrane. In guinea pig brain membrane K4 and K6 stimulated G-protein, the efficacy of K4 was inhibited by nor-BNI, while the effect of K6 was not. K6 exhibited a strong antinociceptive effect in formalin test

Egy kvalitatív kutatás eredményei a dél-alföldi régió egyes mezőgazdasági vállalkozásainál

In 2004 Hungary ha s afiiliated to the European Union. The country has been the part of a big economic integration. The (agri)products ofth e other counlries can flow without bordér. In our work \ve wa s wondered the effect of the connection to EU. In our investigation we made seven deep interviews with managers of the Hungárián agricultural, or food enterprises about the changes

Egy kvalitatív kutatás eredményei a dél-alföldi régió egyes mezőgazdasági vállalkozásainál

In 2004 Hungary ha s afiiliated to the European Union. The country has been the part of a big economic integration. The (agri)products ofth e other counlries can flow without bordér. In our work we was wondered the effect of the connection to EU. In our investigation we made seven deep interviews with managers of the Hungárián agricultural, or food enterprises about the changes

Útvonalfüggő kockázatvállalás A korábbi nyereség és a kockázatvállalás abszolút szintje közötti kapcsolat egy banki ügyfélportfólió adatbázisán

A szakirodalom alapján összefoglaltuk, hogy milyen összefüggés állhat fenn a korábbi nyereségek és a kockázatvállalási hajlandóság között, majd egy hazai banki adatbázison megvizsgáltuk, hogy a vállalati és intézményi ügyfelek elmúlt időszakban elért nyeresége mennyiben magyarázza a kockázati kitettség abszolút szintjét az EUR/HUF devizapárban 2008 és 2012 között havi időskálán. Azt kaptuk, hogy a veszteségek szignifikánsan negatív, míg a nyereségek enyhén pozitív kapcsolatban állnak a kitettség szintjével. Ez a V-alakú összefüggés konzisztens a kilátáselmélettel, különösen a küszöbérték-hatással és a házpénze-hatással. Mivel az irracionális (viselkedési) hatások egyéni és rendszerszinten is értékrombolók lehetnek, mind a befektetőknek, mind a szabályozónak érdemes figyelmet fordítaniuk erre a jelenségre

Irrational risk‑taking of professionals? The relationship between risk exposures and previous profts

The risk attitude of investors is a key factor determining fnancial asset prices and market trends. Changes in risk attitude may be due to the interference of macro-level (business cycle) and micro-level (individual experience) efects. We investigate the impact of individual experience on the subsequent risk-taking attitude of professionals via the analysis of the trading activity of 351 non-fnancial frms and (non-bank) fnancial institutions (insurance companies, fnancial intermediaries, etc.) covering 57,039 FX forward transactions in a highly volatile period between January 2008 and November 2012. Panel regressions for all frms and institutions do not show signifcant behavioral patterns. When investigating each client separately, however, we fnd that 39.7% of the clients having enough transactions to analyze statistically tend to increase their risk exposure irrationally after large gains or losses which can be the manifestation of the break-even and house-money efects well-documented in the literature for non-professionals. This irrational behavior may destroy value, so both market players and regulators should pay attention to monitor and control it

Food-inspired peptides from spinach Rubisco endowed with antioxidant, antinociceptive and anti-inflammatory properties

Rubiscolin-6 (amino acid sequence: YPLDLF) is a selective & delta;-opioid receptor peptide isolated from spinach Rubisco. Its synthetic analogue, peptide YPMDIV is the most potent described so far for its increased opioid activity, thus in this work it was considered as lead compound for the design of twelve new analogues e.g. LMAS112. Firstly all the novel compounds have been tested for their antinociceptive and anti-inflammatory capacity in vitro and in vivo in order to evaluate their ability to maintain or loss the original activity. Among them peptides LMAS5-8 gave the best results, thus their antioxidant properties have been investigated along with their enzymatic inhibitory ability. Peptide LMAS6 shows a strong antioxidant (154.25 mg TE/g CUPRAC) and inhibitor activity on tyrosinase (84.49 mg KAE/g), indicating a potential role in food industry as anti-browning agent, while peptides LMAS5 and LMAS7 possess a modest cholinesterase inhibitory activity suggesting a conceivable use for nutraceuticals production