Search results for "Mimetics"
showing 10 items of 120 documents
New Fluorinated Peptidomimetics through Tandem Aza-Michael Addition to α-Trifluoromethyl Acrylamide Acceptors: Synthesis and Conformational Study in …
2009
A range of partially modified retro (PMR) psi[NHCH(2)] peptide mimetics containing a hydrolytically stable CH(2)CH(CF(3))CO unit have been synthesized. The first kind of peptidomimetics is obtained from the highly efficient aza-Michael addition of different amines to alpha-trifluoromethyl acrylamide acceptors. Subsequent deprotection of the amino group furnishes the key common intermediate for the synthesis of other families of peptidomimetics: dipeptides, tripeptides, peptidomimetics containing a urea moiety, and structures containing two units of alpha-trifluoromethyl-beta(2)-alanine. Finally, a conformational study of several of the newly synthesized peptidomimetics, performed with the a…
Characterization of sensory neurotransmission and its inhibition via alpha 2B-adrenoceptors and via non-alpha 2-receptors in rabbit iris.
1993
To find out whether, and which type of, adrenoceptors mediate prejunctional inhibition of sensory neurotransmitter release from trigeminal fibres, the modulation of twitch response to electrical field stimulation on rabbit isolated iris was investigated. Evoked iris sphincter contractions consisted of a minor fast cholinergic and a large slow component. The latter was unaffected by atropine and guanethidine, hence nonadrenergic noncholinergic in nature (NANC), but nearly completely abolished by capsaicin pretreatment and by the neurokinin receptor antagonist spantide. The response was probably not mediated by NK2 receptors as SR 48,968, an NK2 selective nonpeptide antagonist, failed to redu…
Design, Synthesis, and Biological Evaluation of Novel Fluorinated Ethanolamines
2011
The preparation of novel fluorinated allylamines and their use as key fragments for the stereoselective synthesis of hydroxyethyl secondary amine (HEA)-type peptidomimetics is described. Our strategy employs chiral sulfinyl imines as synthesis intermediates, by treatment of hemiaminal precursors with two equivalents of vinylmagnesium bromide. The subsequent oxidation of the allylic amines to the corresponding epoxides was achieved by treatment with methyl(trifluoromethyl)dioxirane. Finally, epoxide ring opening with a range of nitrogen nucleophiles provided a library of HEA-derived peptidomimetics with a phenyldifluoromethylene moiety. The biological evaluation of these derivatives revealed…
An ontology for cognitive mimetics
2018
AI and autonomous systems are intended to replace people in several jobs. People have worked in these jobs being able to execute the required information processing. This implies that new technical artefacts must be able to perform equitably effective information processing. Thus, it makes sense to develop the analysis of human information processing in designing intelligent systems. This approach has been termed cognitive mimetics. This paper studies how it would be practical to gain knowledge about human information processing and organize this knowledge using ontologies.
Questions in Cognitive Mimetics
2021
Human thinking advances through questions and answers. Any field of human endeavor is permeated by the presence of questions, answers and presuppositions. Questions have a kind of universality, whereby one can place the question marks on anything, including questions themselves. The process of asking the right questions about the right things and in the right way are key for the explication of an approach. Recently, we have begun thinking about an approach to the design of intelligent technology: Cognitive mimetics. In brief, the idea is to take inspiration of empirical human thinking in specific contexts to develop AI solutions. The purpose of this article is to question this approach from…
A spiking network for body size learning inspired by the fruit fly
2013
The concept of peripersonal space is an interesting research topics for psychologists, neurobiologists and for robotic applications. A living being can learn the representation of its own body to take the correct behavioral decision when interacting with the world. To transfer these important learning mechanisms on bio-robots, simple and efficient solutions can be found in the insect world. In this paper a neural-based model for body-size learning is proposed taking into account the results obtained in experiments with fruit flies. Simulations and experimental results on a roving platform are reported and compared with the biological counterpart.
Effects of several muscarinic agonists on cardiac performance and the release of noradrenaline from sympathetic nerves of the perfused rabbit heart
1972
Summary 1 The effects of several muscarinic agonists on atrial tension development, ventricular rate and noradrenaline release from terminal sympathetic fibres evoked by electrical nerve stimulation (SNS) and 1,1-dimethyl-4-phenylpiperazinium (DMPP) were measured in isolated perfused rabbit hearts. 2 Hexamethonium, in a concentration which almost abolished the release of noradrenaline by DMPP, had no effect on the release produced by SNS, confirming that the stimulation was postganglionic. 3 The order of potency for inhibition of atrial tension development was N-methyl-1,2,5,6, tetrahydro-nicotinic acid prop-2-yne ester (MH-1)>oxotremorine > acetylcholine > methacholine > carbachol > furtre…
A muscarinic inhibition of the noradrenaline release evoked by postganglionic sympathetic nerve stimulation
1969
1. The noradrenaline output from isolated rabbit hearts perfused with Tyrode solution was estimated fluorimetrically. The postganglionic sympathetic nerves of the heart were stimulated (10 shocks/sec; 1 msec) for three 1 min periods with intervals of 10 min. 2. The noradrenaline output evoked by 3 consecutive stimulation periods decreased exponentially. 3. Acetylcholine (10−9–10−6 g/ml) administered continuously one min before to one min after the second stimulation caused a dose-dependent reduction of the noradrenaline output evoked by the second stimulation to as low as 19% of the normal value. Acetylcholine in the concentrations applied did not cause a noradrenaline output by itself. 4. …
Absence of muscarinic modulation of vasopressin release from the isolated rat neurohypophysis
1975
1. Isolated rat neurohypophyses were incubated in Locke solution at 37°C and the vasopressin output into the medium determined by bioassay. 2. Potassium chloride 60 mM caused a 9-fold increase in the rate of vasopressin release that was abolished when calcium chloride was omitted from the Locke solution. 3. Acetylcholine 5.5×10−4 M neither alone nor in the presence of atropine 2.9×10−6 M changed the “resting” release of vasopressin. 4. Neither acetylcholine 5.5×10−4 M nor oxotremorine 10−4 and 3×10−4 M altered the vasopressin release evoked by potassium chloride 60 mM. 5. In contrast to the peripheral adrenergic nerve fibres, the secretory terminal fibres of the neurohypophysis do not appea…
Adaptive Materials Research for Architecture
2018
The volume "Adaptive Materials Research for Architecture" is a Special Issue of the journal "Advanced Material Research". The goal of this volume is to spread knowledge on studies, analyses and results of scientific research carried out from academics, researchers, and scientists regarding the soundest issues related to smart materials, innovative technologies and ongoing researches in the field of adaptive materials in past and current architectural practice.