{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,23]],"date-time":"2026-06-23T07:39:25Z","timestamp":1782200365506,"version":"3.54.5"},"reference-count":25,"publisher":"S. Karger AG","issue":"3-4","license":[{"start":{"date-parts":[[2018,1,1]],"date-time":"2018-01-01T00:00:00Z","timestamp":1514764800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/www.karger.com\/Services\/SiteLicenses"},{"start":{"date-parts":[[2018,1,1]],"date-time":"2018-01-01T00:00:00Z","timestamp":1514764800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.karger.com\/Services\/SiteLicenses"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmacology"],"published-print":{"date-parts":[[2018]]},"abstract":"<jats:p>&lt;b&gt;&lt;i&gt;Background:&lt;\/i&gt;&lt;\/b&gt; Drotaverine, a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor, blocks the degradation of 3\u2019,5\u2019-cyclic adenosine monophosphate. However, published receptor binding data showed that drotaverin also binds to the L-type voltage-operated calcium channel (L-VOCC). Based on these molecular mechanisms of action, a direct and indirect (by blocking the constrictor response) relaxant effect on airway smooth muscle can be predicted, which has not yet been assessed. &lt;b&gt;&lt;i&gt;Summary:&lt;\/i&gt;&lt;\/b&gt; Accordingly, drotaverine and reference agents were tested both on the histamine-, methacholine-, or KCl-induced contraction response and on precontracted guinea pig tracheal preparations. It was found that drotaverine not only relaxed the precontracted tracheal preparations but also decreased mediator-induced contraction. These effects of drotaverine were concentration dependent, with a significantly higher potency on the KCl-induced response, than on either the histamine or methacholine induced one. A similar result was noted for nifedipine. The PDE inhibitor, theophylline, also relaxed the precontracted preparations but was ineffective on the mediator-induced contraction in a physiologically relevant concentration range. Moreover, theophylline did not show selectivity and was the least potent relaxant among the 3 tested molecules. &lt;b&gt;&lt;i&gt;Key Message:&lt;\/i&gt;&lt;\/b&gt; These results show that drotaverine is a more potent airway smooth muscle relaxant molecule than theophylline. This enhanced potency on relaxation and inhibition of the constrictor response, at least partly, may be explained by the combined L-VOCC blocking and PDE inhibitory potential of drotaverine.<\/jats:p>","DOI":"10.1159\/000485921","type":"journal-article","created":{"date-parts":[[2018,1,4]],"date-time":"2018-01-04T22:06:26Z","timestamp":1515103586000},"page":"163-169","source":"Crossref","is-referenced-by-count":4,"title":["Assessment of the Airway Smooth Muscle Relaxant Effect of Drotaverine"],"prefix":"10.1159","volume":"101","author":[{"given":"Zolt\u00e1n","family":"Patai","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andr\u00e1s","family":"Guttman","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Endre\u00a0G.","family":"Mikus","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"127","published-online":{"date-parts":[[2018,1,4]]},"reference":[{"key":"ref1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(02)01993-3"},{"key":"ref2","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1984.tb10812.x"},{"key":"ref3","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1985.tb17380.x"},{"key":"ref4","doi-asserted-by":"publisher","DOI":"10.1152\/ajplung.1994.266.6.L620"},{"key":"ref5","doi-asserted-by":"publisher","DOI":"10.1124\/jpet.116.237271"},{"key":"ref6","doi-asserted-by":"publisher","DOI":"10.1111\/j.2042-7158.1990.tb05362.x"},{"key":"ref7","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(91)90480-E"},{"key":"ref8","doi-asserted-by":"publisher","DOI":"10.1254\/jphs.FPJ05013X"},{"key":"ref9","doi-asserted-by":"publisher","DOI":"10.1152\/ajplung.1996.271.2.L300"},{"key":"ref10","doi-asserted-by":"publisher","DOI":"10.3390\/ph3030725"},{"key":"ref11","doi-asserted-by":"publisher","DOI":"10.1111\/j.1365-2885.2007.00904.x"},{"key":"ref12","doi-asserted-by":"publisher","DOI":"10.1152\/ajpcell.1991.261.3.C497"},{"key":"ref13","doi-asserted-by":"publisher","DOI":"10.1152\/ajpcell.1993.265.4.C877"},{"key":"ref14","doi-asserted-by":"publisher","DOI":"10.1016\/S0024-3205(99)00152-6"},{"key":"ref15","doi-asserted-by":"publisher","DOI":"10.1378\/chest.86.4.515"},{"key":"ref16","doi-asserted-by":"publisher","DOI":"10.1164\/ajrccm\/136.1.76"},{"key":"ref17","doi-asserted-by":"publisher","DOI":"10.1016\/0091-6749(87)90247-8"},{"key":"ref18","doi-asserted-by":"publisher","DOI":"10.1046\/j.0306-5251.2001.01560.x"},{"key":"ref19","doi-asserted-by":"publisher","DOI":"10.1016\/j.pupt.2012.05.007"},{"key":"ref20","doi-asserted-by":"publisher","DOI":"10.1016\/j.pupt.2012.05.007"},{"key":"ref21","doi-asserted-by":"publisher","DOI":"10.1053\/prrv.2000.0102"},{"key":"ref22","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejphar.2005.12.059"},{"key":"ref23","doi-asserted-by":"publisher","DOI":"10.1152\/physrev.1994.74.2.365"},{"key":"ref24","doi-asserted-by":"publisher","DOI":"10.1007\/978-3-642-13443-2_17"},{"key":"ref25","doi-asserted-by":"publisher","DOI":"10.1007\/164_2016_71"}],"container-title":["Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.karger.com\/Article\/Pdf\/485921","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.karger.com\/Article\/Pdf\/485921","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,4,23]],"date-time":"2025-04-23T16:28:53Z","timestamp":1745425733000},"score":1,"resource":{"primary":{"URL":"https:\/\/karger.com\/article\/doi\/10.1159\/000485921"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2018]]},"references-count":25,"journal-issue":{"issue":"3-4","published-online":{"date-parts":[[2018,2,23]]},"published-print":{"date-parts":[[2018,2,20]]}},"URL":"https:\/\/doi.org\/10.1159\/000485921","archive":["Portico"],"relation":{},"ISSN":["0031-7012","1423-0313"],"issn-type":[{"value":"0031-7012","type":"print"},{"value":"1423-0313","type":"electronic"}],"subject":[],"published":{"date-parts":[[2018]]}}}