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Atypical sympathomimetic drug lerimazoline mediates contractile effects in rat aorta predominantly by 5-HT2A receptors
dc.creator | Rizvic, Eldina | |
dc.creator | Jankovic, Goran | |
dc.creator | Kostić Rajačić, Slađana | |
dc.creator | Savić, Miroslav M. | |
dc.date.accessioned | 2019-01-30T17:54:42Z | |
dc.date.available | 2019-01-30T17:54:42Z | |
dc.date.issued | 2017 | |
dc.identifier.issn | 1512-8601 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/2161 | |
dc.description.abstract | Lerimazoline is a sympathomimetic drug that belongs to the imidazoline class of compounds, and is used as a nasal decongestant. Studies on lerimazoline are rare, and its pharmacological profile is not completely understood. Here, we analyzed the affinity of lerimazoline for dopamine receptor D2, serotonin 5-HT1A and 5-HT2A receptors and alpha(1)-adrenoceptor, and investigated lerimazoline contractile effects in isolated rat thoracic aorta. We also determined the effect of several antagonists on the contractile response to lerimazoline, including prazosin (alpha(1)-adrenoceptor antagonist), RX 821002 and rauwolscine (alpha(2)-adrenoceptor antagonists), JP 1302 (alpha(2C)-adrenoceptor antagonist), methiothepin (non-selective 5-HT receptor antagonist), SB 224289 (5-HT1B receptor antagonist), BRL 15572 (5-HT1D receptor antagonist), and ketanserin (5-HT2A receptor antagonist). Lerimazoline displayed high affinity for the 5-HT1A receptor (Ki = 162.5 nM), similar to the previously reported affinity for the 5-HT1D receptor. Binding affinity estimates (Ki) for alpha(1), 5-HT2A, and D-2 receptors were 6656, 4202 and 3437.5 nM, respectively (the literature reported Ki for 5-HT1B receptor is 3480 nM). Lerimazoline caused concentration-dependent contractions in 70% of preparations, varying in the range between 40% and 55% of the maximal contraction elicited by phenylephrine. While prazosin reduced the maximum contractile response to lerimazoline, rauwolscine showed a non-significant trend in reduction of the response. Both ketanserin (10 nM and 1 mu M) and methiothepin strongly suppressed the maximum response to lerimazoline. Overall, our results suggest that 5-HT2A and, less distinctly, alpha(1)-adrenergic receptors are involved in the lerimazoline-induced contractions, which makes lerimazoline an "atypical" decongestant. | en |
dc.publisher | Association of Basic Medical Sciences of Federation of Bosnia and Herzegovina | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175076/RS// | |
dc.rights | openAccess | |
dc.source | Bosnian Journal of Basic Medical Sciences | |
dc.subject | Lerimazoline | en |
dc.subject | rat aorta | en |
dc.subject | binding affinity | en |
dc.subject | phenylephrine | en |
dc.subject | 5-HT2A receptors | en |
dc.subject | St-71 | en |
dc.subject | trimizoline | en |
dc.subject | tramazoline | en |
dc.subject | antagonist activity | en |
dc.subject | sympathomimetic drug | en |
dc.title | Atypical sympathomimetic drug lerimazoline mediates contractile effects in rat aorta predominantly by 5-HT2A receptors | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Савиц, Мирослав М.; Костић Рајачић, Слађана; Ризвиц, Елдина; Јанковиц, Горан; | |
dc.citation.volume | 17 | |
dc.citation.issue | 3 | |
dc.citation.spage | 194 | |
dc.citation.epage | 202 | |
dc.citation.other | 17(3): 194-202 | |
dc.citation.rank | M23 | |
dc.identifier.pmid | 28628756 | |
dc.identifier.doi | 10.17305/bjbms.2017.2071 | |
dc.identifier.fulltext | https://cer.ihtm.bg.ac.rs//bitstream/id/8575/2159.pdf | |
dc.identifier.scopus | 2-s2.0-85028598122 | |
dc.identifier.wos | 000410590500003 | |
dc.type.version | publishedVersion |