Gabriella De Martino , Giuseppe La Regina , Francesco La Torre , Roberto Cirilli , Ilario Mereghetti , Alfredo Cagnotto , Marino Artico , Romano Silvestri
{"title":"1,3,4,14b-四氢-2,10-二甲基- 2h, 10h -吡嗪基[2,1-d]吡咯基[1,2-b][1,2,5]苯并三氮卓(10-甲基-10-氮唑他平)和2-甲基-1,3,4,14b-四氢- 2h -吡嗪基[2,1-d]吡咯基[1,2-b][1,2,5]苯并噻二氮卓- 10,10-二氮卓(硫唑他平)的手性拆分和结合研究","authors":"Gabriella De Martino , Giuseppe La Regina , Francesco La Torre , Roberto Cirilli , Ilario Mereghetti , Alfredo Cagnotto , Marino Artico , Romano Silvestri","doi":"10.1016/j.farmac.2005.07.007","DOIUrl":null,"url":null,"abstract":"<div><p>The affinities of the enantiomers of 1,3,4,14b-tetrahydro-2,10-dimethyl-2<em>H</em>,10<em>H</em>-pyrazino[2,1-<em>d</em>]pyrrolo[1,2-<em>b</em>] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine, <strong>5</strong>) and 2-methyl-1,3,4,14b-tetrahydro-2<em>H</em>-pyrazino[2,1-<em>d</em>]pyrrolo[1,2-<em>b</em>] [1,2,5]benzothiadiazepine 10,10-dioxide (tiaaptazepine, <strong>6</strong>) were evaluated in receptor binding assays. Compound (+)-(S)-<strong>5</strong>, the most significant tested enantiomer, showed good affinities for 5-HT<sub>1A</sub>, 5-HT<sub>2A</sub> 5-HT<sub>2C</sub> and α<sub>2NA</sub> receptors, moderate affinities for DA<sub>1</sub>, DA<sub>3r</sub> and 5-HT<sub>3</sub> receptors and it was devoid of affinity for DA<sub>2</sub>, α<sub>1NA</sub><span> and muscarinic receptors. Compound (+)-(S)-</span><strong>5</strong><span><span> showed an interesting pharmacological profile different from those of the reference compounds mirtazepine, </span>mianserin and 6-methoxymianserin.</span></p></div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 11","pages":"Pages 931-937"},"PeriodicalIF":0.0000,"publicationDate":"2005-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.07.007","citationCount":"3","resultStr":"{\"title\":\"Chiral resolution and binding study of 1,3,4,14b-tetrahydro-2,10-dimethyl-2H,10H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine) and 2-methyl-1,3,4,14b-tetrahydro-2H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzothiadiazepine 10,10-dioxide (tiaaptazepine)\",\"authors\":\"Gabriella De Martino , Giuseppe La Regina , Francesco La Torre , Roberto Cirilli , Ilario Mereghetti , Alfredo Cagnotto , Marino Artico , Romano Silvestri\",\"doi\":\"10.1016/j.farmac.2005.07.007\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The affinities of the enantiomers of 1,3,4,14b-tetrahydro-2,10-dimethyl-2<em>H</em>,10<em>H</em>-pyrazino[2,1-<em>d</em>]pyrrolo[1,2-<em>b</em>] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine, <strong>5</strong>) and 2-methyl-1,3,4,14b-tetrahydro-2<em>H</em>-pyrazino[2,1-<em>d</em>]pyrrolo[1,2-<em>b</em>] [1,2,5]benzothiadiazepine 10,10-dioxide (tiaaptazepine, <strong>6</strong>) were evaluated in receptor binding assays. Compound (+)-(S)-<strong>5</strong>, the most significant tested enantiomer, showed good affinities for 5-HT<sub>1A</sub>, 5-HT<sub>2A</sub> 5-HT<sub>2C</sub> and α<sub>2NA</sub> receptors, moderate affinities for DA<sub>1</sub>, DA<sub>3r</sub> and 5-HT<sub>3</sub> receptors and it was devoid of affinity for DA<sub>2</sub>, α<sub>1NA</sub><span> and muscarinic receptors. Compound (+)-(S)-</span><strong>5</strong><span><span> showed an interesting pharmacological profile different from those of the reference compounds mirtazepine, </span>mianserin and 6-methoxymianserin.</span></p></div>\",\"PeriodicalId\":77128,\"journal\":{\"name\":\"Farmaco (Societa chimica italiana : 1989)\",\"volume\":\"60 11\",\"pages\":\"Pages 931-937\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2005-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/j.farmac.2005.07.007\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Farmaco (Societa chimica italiana : 1989)\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0014827X05001588\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Farmaco (Societa chimica italiana : 1989)","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0014827X05001588","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Chiral resolution and binding study of 1,3,4,14b-tetrahydro-2,10-dimethyl-2H,10H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine) and 2-methyl-1,3,4,14b-tetrahydro-2H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzothiadiazepine 10,10-dioxide (tiaaptazepine)
The affinities of the enantiomers of 1,3,4,14b-tetrahydro-2,10-dimethyl-2H,10H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine, 5) and 2-methyl-1,3,4,14b-tetrahydro-2H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzothiadiazepine 10,10-dioxide (tiaaptazepine, 6) were evaluated in receptor binding assays. Compound (+)-(S)-5, the most significant tested enantiomer, showed good affinities for 5-HT1A, 5-HT2A 5-HT2C and α2NA receptors, moderate affinities for DA1, DA3r and 5-HT3 receptors and it was devoid of affinity for DA2, α1NA and muscarinic receptors. Compound (+)-(S)-5 showed an interesting pharmacological profile different from those of the reference compounds mirtazepine, mianserin and 6-methoxymianserin.
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