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dc.creatorRizvić, Eldina
dc.creatorJanković, Goran
dc.creatorKostić-Rajacić, Sladana
dc.creatorSavić, Miroslav
dc.date.accessioned2019-09-02T11:57:14Z
dc.date.available2019-09-02T11:57:14Z
dc.date.issued2017
dc.identifier.issn1512-8601
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/2790
dc.description.abstractLerimazoline 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.publisherAssoc Basic Medical Sci Federation Bosnia & Herzegovina Sarajevo, Cekalusa
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175076/RS//
dc.rightsopenAccess
dc.sourceBosnian Journal of Basic Medical Sciences
dc.titleAtypical sympathomimetic drug lerimazoline mediates contractile effects in rat aorta predominantly by 5-HT2A receptorsen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractКостић-Рајацић, Сладана; Јанковић, Горан; Савић, Мирослав; Ризвић, Елдина;
dc.citation.volume17
dc.citation.issue3
dc.citation.spage194
dc.citation.epage202
dc.citation.other17(3): 194-202
dc.citation.rankM23
dc.identifier.wos000410590500003
dc.identifier.doi10.17305/bjbms.2017.2071
dc.identifier.pmid28628756
dc.identifier.scopus2-s2.0-85028598122
dc.identifier.fulltexthttp://farfar.pharmacy.bg.ac.rs//bitstream/id/1429/2788.pdf
dc.identifier.rcubconv_3941
dc.type.versionpublishedVersion


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