55 research outputs found

    Prikaz koronarnih arterija ovce na anatomskom preparatu srca primjenom poliuretanske smjese

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    Dijagnostika bolesti koronarnih arterija i primjena odgovarajuće terapije u porastu je u veterinarskoj medicini. U svrhu ispravnog pristupa bolestima koronarnih arterija nužno je prethodno znanje o njihovoj anatomskoj građi, posebno položaju i grananju. Tijekom anatomske sekcije srca, položaj i grananje koronarnih arterija teško je proučiti ako prethodno nisu ispunjene određenim punilom. U svrhu boljeg prikaza ogranaka koronarnih arterija u njihov smo lumen injektirali smjesu poliuretanskog laka i crvenog praškastog pigmenta. Nakon sekcije koronarnih arterija opisali smo njihovo grananje na modelu ovce i uočili odstupanja od opisa u literaturi te ističemo važnost poznavanja anatomskih varijacija među vrstama, ali i među jedinkama iste vrste

    Prikaz koronarnih arterija ovce na anatomskom preparatu srca primjenom poliuretanske smjese

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    Dijagnostika bolesti koronarnih arterija i primjena odgovarajuće terapije u porastu je u veterinarskoj medicini. U svrhu ispravnog pristupa bolestima koronarnih arterija nužno je prethodno znanje o njihovoj anatomskoj građi, posebno položaju i grananju. Tijekom anatomske sekcije srca, položaj i grananje koronarnih arterija teško je proučiti ako prethodno nisu ispunjene određenim punilom. U svrhu boljeg prikaza ogranaka koronarnih arterija u njihov smo lumen injektirali smjesu poliuretanskog laka i crvenog praškastog pigmenta. Nakon sekcije koronarnih arterija opisali smo njihovo grananje na modelu ovce i uočili odstupanja od opisa u literaturi te ističemo važnost poznavanja anatomskih varijacija među vrstama, ali i među jedinkama iste vrste

    Sinteza i farmakološko ispitivanje (±)-2,3-seco-analoga fentanila

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    An efficient, five-step synthetic approach to various acyclic 1,3-diamines has been developed and applied to the preparation of a novel class of open-chained fentanyl analogues. The acyclic derivatives 5.1-5.5 (all new compounds) were synthesized with the aim of estimating the significance of the piperidine ring for the opioid analgesic activity of anilido-piperidines. The starting beta-keto-amide 1.1, prepared by the aminolysis of methyl acetoacetate with methyl phenethylamine, (93% yield), was successively reacted with NaH and BuLi, to form the highly reactive alpha,gamma-dienolate anion 1.1a. Regio and chemoselective gamma-alkylation of the dienolate with various primary and secondary alkyl halides furnished the beta-keto-amides 1.2-1.5 (76-91%). Reductive amination of the keto-amides 1.1-1.5 with aniline and Zn powder in acetic acid, via the enamine intermediates 2.1-2.5. afforded the beta-anilino amides 3.1-3.5 (74-85%). After reductive deoxygenation of the tertiary amide group, using in situ generated diborane, the corresponding 1,3-diamines 4.1-4.5 were obtained (87-97%). The synthesis of (+/-)-2,3-seco-fentanyls 5.1-5.5 was completed by N-acylation of the diamines 4.1-4.5 with propionyl chloride, followed by precipitation of the monooxalate salts (86-95%). The parent compound, 2,3-seco-fentanyl 5.1, was found to be a 40 times less potent narcotic analgesic than fentanyl but still 5-6 times more active than morphine in rats. while i-Pr derivative 5.3 was inactive. Apart from the pharmacological significance. the general procedure described herein may afford various functionalized, 1,3-diamines as potential complexing agents and building blocks for the synthesis of aza-crown ethers.Razvijen je efikasan postupak za dobijanje različitih acikličnih 1,3-diamina u pet faza, i primenjen u sintezi nove klase analoga fentanila otvorenog niza. Derivati 5.1–5.5 (svi su nova jedinjenja) sintetisani su sa ciljem da se proceni uticaj piperidinskog prstena na opioidnoanalgetičku aktivnost anilido-piperidina. Polazni β-keto-amid 1.1, dobijen aminolizom metilacetoacetata metilfenetilaminom (prinos 93 %), bio je sukcesivno tretiran sa NaH i BuLi, pri čemu je postao veoma reaktivni α,γ-dienolatni anjon 1.1a. Regio- i hemoselektivnim γ-alkilovanjem ovog dienolata različitim primarnim i sekundarnim alkil-halogenidima, dobijeni su β-keto-amidi 1.2–1.5 (prinos 76–91 %). Reduktivnim aminovanjem keto-amida 1.1–1.5 pomoću Zn praha i sirćetne kiseline, preko enaminskih intermedijera 2.1–2.5, postali su -anilino-amidi 3.1–3.5 (prinos 74–85 %). Posle reduktivne deoksigenacije tercijene amidne funkcije, koristeći in situ generisani diboran, odgovarajući 1,3-diamini 4.1–4.5 izolovani su u prinosima 87–97 %. Sinteza (±)-2,3-seco-fentanila 5.1–5.5 završena je N-acilovanjem diamina 4.1–4.5 propionil-hloridom, a zatim taloženjem u obliku monooksalatnih soli (prinos 86–95 %). Nađeno je da je osnovno jedinjenje, 2,3-seco fentanil 5.1, 40 puta slabiji narkotički analgetik od fentanila, ali još uvek 5–6 puta aktivniji od morfina u pacova, dok je i-Pr derivat 5.3 bio neaktivan. Osim farmakološkog značaja, opštim postupkom prikazanim u ovom radu, mogu se sintetisati različiti 1,3-diamini, uključujući i one sa funkcionalnim grupama. Ova jedinjenja mogu biti potencijalno značajna kao kompleksirajući agensi i kao intermedijeri u sintezi aza-kraun-etara

    On the word problem for SP-categories, and the properties of two-way communication

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    International audienceThe word problem for categories with free products and coproducts (sums), SP-categories, is directly related to the problem of determining the equivalence of certain processes. Indeed, the maps in these categories may be directly interpreted as processes which communicate by two-way channels. The maps of an SP-category may also be viewed as a proof theory for a simple logic with a game theoretic intepretation. The cut-elimination procedure for this logic determines equality only up to certain permuting conversions. As the equality classes under these permuting conversions are finite, it is easy to see that equality between cut-free terms (even in the presence of the additive units) is decidable. Unfortunately, this does not yield a tractable decision algorithm as these equivalence classes can contain exponentially many terms. However, the rather special properties of these free categories -- and, thus, of two-way communication -- allow one to devise a tractable algorithm for equality. We show that, restricted to cut-free terms s,t : X --> A, the decision procedure runs in time polynomial on |X||A|, the product of the sizes of the domain and codomain type

    Synthesis, characterization and cytotoxicity of a palladium(II) complex of 3-[(2-hydroxybenzylidene)amino]-2-thioxoimidazolidin-4-one

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    The polydentate ligand 3-[(2-hydroxybenzylidene)amino]-2-thioxoimidazolidin-4-one was synthesized in the intermolecular cyclocondensation reaction of 2-hydroxybenzaldehyde thiosemicarbazone and ethyl chloroacetate. A novel palladium(II) complex was obtained from cis-[Pd(DMSO)(2)Cl-2] by nucleophilic substitution of both DMSO ligands with the iminic nitrogen and the thiolactamic sulfur from the ligand. The structures of the compounds were characterized based on their spectral data. The cytotoxic activities of the ligand and the palladium(II) complex were studied on the tumor cell lines: human colon carcinoma HCT-116 and SW-480 cells using the MTT viability test. The results showed that the investigated palladium(II) complex had a significantly greater cytotoxic effect compared to that of the ligand

    Pharmacological evaluation of 3-carbomethoxy fentanyl in mice

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    In many animal species, as well as in humans, high doses of fentanyl (F) produce marked neurotoxic effects, such as muscular rigidity and respiratory depression. The antinociception (hot-plate test), impairment of motor coordination (rotarod test) and acute toxicity of intraperitoneal newly synthesized analogs, (±)cis-3-carbomethoxy- fentanyl (C) and (±)trans-3-carbomethoxyfentanyl (T) were evaluated in mice. The compounds tested induced antinociception, impairment of performance on the rotarod, and lethality in a dosedependent manner. The relative order of antinociceptive potency was similar to motor impairment potency, as well as lethality: F gt C gt T. Naloxone hydrochloride (1 mg/kg; sc) abolished all the effects observed, suggesting that they are mediated via opioid receptors, most probably of μ type. There were no significant differences between the therapeutic indices of F, C and T. It is concluded, the introduction of 3-carbomethoxy group in the piperidine ring of the fentanyl skeleton reduced the potency, but did not affect tolerability and safety of the compound. © 2011 by the authors

    Permutonestohedra

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    There are several real spherical models associated with a root arrangement, depending on the choice of a building set. The connected components of these models are manifolds with corners which can be glued together to obtain the corresponding real De Concini–Procesi models. In this paper, starting from any root system with finite Coxeter group W and any W -invariant building set, we describe an explicit realization of the real spherical model as a union of polytopes (nestohedra) that lie inside the chambers of the arrangement. The main point of this realization is that the convex hull of these nestohedra is a larger polytope, a permutonestohedron, equipped with an action of W or also, depending on the building set, of Aut ( ). The permutonestohedra are natural generalizations of Kapranov’s permutoassociahedra

    Cognitive vision system for control of dexterous prosthetic hands: Experimental evaluation

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    <p>Abstract</p> <p>Background</p> <p>Dexterous prosthetic hands that were developed recently, such as SmartHand and i-LIMB, are highly sophisticated; they have individually controllable fingers and the thumb that is able to abduct/adduct. This flexibility allows implementation of many different grasping strategies, but also requires new control algorithms that can exploit the many degrees of freedom available. The current study presents and tests the operation of a new control method for dexterous prosthetic hands.</p> <p>Methods</p> <p>The central component of the proposed method is an autonomous controller comprising a vision system with rule-based reasoning mounted on a dexterous hand (CyberHand). The controller, termed cognitive vision system (CVS), mimics biological control and generates commands for prehension. The CVS was integrated into a hierarchical control structure: 1) the user triggers the system and controls the orientation of the hand; 2) a high-level controller automatically selects the grasp type and size; and 3) an embedded hand controller implements the selected grasp using closed-loop position/force control. The operation of the control system was tested in 13 healthy subjects who used Cyberhand, attached to the forearm, to grasp and transport 18 objects placed at two different distances.</p> <p>Results</p> <p>The system correctly estimated grasp type and size (nine commands in total) in about 84% of the trials. In an additional 6% of the trials, the grasp type and/or size were different from the optimal ones, but they were still good enough for the grasp to be successful. If the control task was simplified by decreasing the number of possible commands, the classification accuracy increased (e.g., 93% for guessing the grasp type only).</p> <p>Conclusions</p> <p>The original outcome of this research is a novel controller empowered by vision and reasoning and capable of high-level analysis (i.e., determining object properties) and autonomous decision making (i.e., selecting the grasp type and size). The automatic control eases the burden from the user and, as a result, the user can concentrate on what he/she does, not on how he/she should do it. The tests showed that the performance of the controller was satisfactory and that the users were able to operate the system with minimal prior training.</p
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