Search

The purpose of this article is to demonstrate that English spatial particles which have grammaticalised into telic aspectualisers are not devoid of the image schematic content, which motivates their use in specific contexts. Because aspectual meaning, including telicity, is compositional in nature, which means that it frequently results from the interaction of several linguistic features, it is vital to single out those predicates in which the telicity effect can be attributed solely to the particle, not any other elements of the construction. This can be implemented by adopting the scalar approach, which shows that telicity is entailed by the particle exclusively in a predicate containing an incremental theme verb. Accordingly, the incremental theme verb burn and its five telic particles (up, down, out, off and away) constitute the subject of investigation. The analysis demonstrates that each particle encodes telicity in terms of reaching the GOAL in the SOURCE-PATH-GOAL schema. Conceptual differences in encoding the termination of the burning process result from topological properties of the path construed by each particle under study.

Information sharing has been considered a critical solution against the ever-increasing complexity of cyber-attacks. In this effort Cyber Threat Intelligence is undergoing a process of increasing its maturity levels. The quantification of the quality of shared information and the assessment of trust amongst information sharing entities is an important part of the process. The Trust and Quality Tool has been designed as a tool with the aim of improving the trust in the relevancy of shared information by enabling an option to assess its trustworthiness and defining a set of metrics for trust and quality.

This paper constitutes an attempt to describe the early stages of morphological development of three Polish children on the basis of the language corpus collected in the form of parental diaries and audio recordings in the course of three-year-long longitudinal studies. The onset of morphological development is accounted for within the framework of Natural Morphology ( Galeas 1998 , Wurzel 1994 , Dressler et al. 1987 ). It is suggested that the premorphological stage is followed by the protomorphological stage which marks the beginning of morphological productivity, which is characterized by a significant degree of constructional iconicity defined by parameters of morphological naturalness, such as diagrammaticity, morphosemantic transparency and transparency of encoding. It is amply demonstrated that the language of children is far more regular than the language of adults due to its tendency to avoid alternation, which goes in line with previous research into the nature of the acquisition of Polish (see e.g. Smoczyńska 1985 ).

This paper investigates the morphological and semantic structure of Polish onomastic derivatives, which became both a medium of journalistic expression and a weapon used in political fight after the year 1989. It is argued that the majority of these eponyms are created by means of foreign affixes, which is seen as a sign of progressing internationalization of Slavic languages, increasingly relying on non-native affixes and derivational patterns. Moreover, the role of the pragmatic context in encoding and decoding these novel coinages is highlighted.

In this study we describe the synthesis and some pharmacological properties of six new analogues of arginine vasopressin (AVP). Five of the peptides were substituted in position 2 with L-1-naphthylalanine (L-1-Nal) or D-1-naphthylalanine (D-1-Nal); one had D-1-Nal in position 3. All analogues were tested in bioassays for pressor and antidiuretic activity. We also tested the uterotonic activity of the peptides in-vitro. Two of the new peptides were moderately potent V1a and oxytocin antagonists. The modifications proposed resulted in a drop or the removal of antidiuretic activity and in the removal of pressor activity, or conversion into moderate antagonists. Two peptides ([Mpa1, (L-1-Nal)2]AVP and [Mpa1, (D-1-Nal)2]AVP) which appear not to interact with V1a and V2 receptors were exceptionally selective oxytocin antagonists in-vitro. These compounds with selective oxytocin antagonistic activity may be promising candidates for the development of potential tocolytic agents for the prevention of pre-term labour.

Six new analogs of arginine-vasopressin, four of them substituted in position 2 with β-thienylalanine and two prolonged on the n-terminus by acylation with 1-adamantaneacetic acid, were synthesized on chloromethylated resin using Boc strategy and DCC or DCC-HOBt to form peptide bond. The activity of the analogs was fairly low, however, one of the peptides, namely [Cpp1, Thi2, Val4]AVP, showed selectivity in antiuterotonic, antipressor and anti-antidiuretic effects.

Eight new compounds were designed, synthesized and bioassayed as a part of our studies on the structure-activity relationship of arginine-vasopresine (AVP) analogs. Tyrosine in position 2 of AVP, dAVP, [Cpp1]AVP and [Cpp1,Val4]AVP was substituted by L-4-chlorophenylalanine (4-Cl-Phe) or D-phenylglycine [D-Gly(Phe)] and the effect of these changes on agonistic/antagonistic activity in uterotonic and pressor test was followed. All but one of these analogs were found inhibitory in uterotonic test, however in most cases their potency was fairly low. As to the pressor activity the agonistic potency of the 4-Cl-Phe substituted analogs was essentially the same as having 4-F-Phe in position 2. As far as the potency of antagonists is concerned, 4-Cl-Phe peptides showed significantly higher potency than the 4-F-Phe analogs. All compounds containing D-phenylglycine in position 2 were inactive in the pressor test.

In an attempt to develop more active and selective analogues of arginine vasopressin (AVP), two peptides have been designed, synthesized and tested for vasopressor (V1-receptors) and antidiuretic (V2-receptors) activities. We also estimated the uterotonic and anti-uterotonic activities of these compounds in-vitro. The first peptide, [(l-2-Nal)3] AVP is a highly active V2-agonist. The second analogue, [(l-2-Nal)3, (d-Arg)8]VP is among the most potent antagonists of the vasopressor response to AVP. Moreover, it is the first V1-antagonist devoid of anti-uterotonic activity. High antipressor potency of the second peptide was achieved without modification of position 1.