Synthesis, characterization and anticonvulsant activity of new series of N-modified analogues of VV-hemorphin-5 with aminophosphonate moiety

Todorov, Petаr; Peneva, Petia; Tchekalarova, Jana; Rangelov, Miroslav; Georgieva, Stela; Todorova, Nadezhda

doi:10.1007/s00726-019-02789-0

Cited by 13 publications

(11 citation statements)

References 47 publications

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“…Importantly, not only the position, but also the nature of the incorporated group had an impact on this phenomenon. The obtained data provide the basis for anticipation that the described compounds may be considered as a promising template for future design of the more active analogues, as well as in studies of other models of epilepsy [52,[89][90][91][92][93].…”

Section: Hemorphin Analoguesmentioning

confidence: 92%

Hemorphins—From Discovery to Functions and Pharmacology

et al. 2021

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During the last three decades, a variety of different studies on bioactive peptides that are opioid receptor ligands, have been carried out, with regard to their isolation and identification, as well as their molecular functions in living organisms. Thus, in this review, we would like to summarize the present state-of-the art concerning hemorphins, methodological aspects of their identification, and their potential role as therapeutic agents. We have collected and discussed articles describing hemorphins, from their discovery up until now, thus presenting a very wide spectrum of their characteristic and applications. One of the major assets of the present paper is a combination of analytical and pharmacological aspects of peptides described by a team who participated in the initial research on hemorphins. This review is, in part, focused on the analysis of endogenous opioid peptides in biological samples using advanced techniques, description of the identification of synthetic/endogenous hemorphins, their involvement in pharmacology, learning, pain and other function. Finally, the part regarding hemorphin analogues and their synthesis, has been added.

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Section: Hemorphin Analoguesmentioning

confidence: 92%

Hemorphins—From Discovery to Functions and Pharmacology

et al. 2021

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“…(5 mL per ventricle) at doses of 0.25, 0.5 and 1 mg, respectively, by means of 28-gauge stainless steel needles attached to 10 mL Hamilton s syringes as described in previous studies. 49,50 The antiseizure effect was evaluated 10 min following the treatment. The doses were chosen based on our previous studies.…”

Section: Voltamperometric Analysismentioning

confidence: 99%

“…The doses were chosen based on our previous studies. [48][49][50][51] 2.4.3. Anticonvulsant activity 2.4.3.1.…”

Section: Voltamperometric Analysismentioning

confidence: 99%

“…39 Based on our previous studies, we showed that hemorphins and their analogues, containing non-proteinogenic and/or natural amino acids, from the N-or C-terminus of the molecules demonstrated dose-and phase-dependent anticonvulsant activity and a lack of neurotoxicity in the rotarod test. [47][48][49][50][51] Our group is one of the leading pioneers in the exploration of anticonvulsant activity of these perspective biopeptides. [47][48][49][50][51] As a natural extension of our research in the synthesis and characterization of new hemorphin analogues as potential anticonvulsants and because of all the above mentioned, herein we illustrated the potential of new N-modified hybrid analogue hemorphins containing a C-5 substituted hydantoin residue as anticonvulsants and inhibitors of sodium channels.…”

Section: Introductionmentioning

confidence: 99%

“…[47][48][49][50][51] Our group is one of the leading pioneers in the exploration of anticonvulsant activity of these perspective biopeptides. [47][48][49][50][51] As a natural extension of our research in the synthesis and characterization of new hemorphin analogues as potential anticonvulsants and because of all the above mentioned, herein we illustrated the potential of new N-modified hybrid analogue hemorphins containing a C-5 substituted hydantoin residue as anticonvulsants and inhibitors of sodium channels. We aimed to synthesize new potent anticonvulsant N-modified hybrid analogues of hemorphins containing a C-5 substituted hydantoin, with proven pharmacological activity, to the peptide fragment.…”

Section: Introductionmentioning

confidence: 99%

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