{"id":13903,"date":"2017-04-28T08:43:32","date_gmt":"2017-04-28T00:43:32","guid":{"rendered":"\/\/www.gsbet888.com\/?p=13903"},"modified":"2019-08-02T18:53:18","modified_gmt":"2019-08-02T10:53:18","slug":"lorcaserin-belviq-%e6%b2%bb%e7%96%97%e8%82%a5%e8%83%96%e7%9a%84%e4%b8%80%e7%a7%8d%e8%8d%af%e7%89%a9","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/molecule\/2017\/04\/lorcaserin-belviq-%e6%b2%bb%e7%96%97%e8%82%a5%e8%83%96%e7%9a%84%e4%b8%80%e7%a7%8d%e8%8d%af%e7%89%a9.html","title":{"rendered":"Lorcaserin (Belviq)\u2014\u6cbb\u7597\u80a5\u80d6\u7684\u4e00\u79cd\u836f\u7269"},"content":{"rendered":"

\u4e00\u3001\u80cc\u666f<\/h4>\n

\u80a5\u80d6\u4e00\u76f4\u662f\u5168\u7403\u6027\u7684\u96be\u9898\uff0c\u7279\u522b\u662f\u5728\u7f8e\u56fd\uff0c\u81f3\u4eca\u90fd\u6ca1\u6709\u4e00\u79cd\u6709\u6548\u7684\u89e3\u51b3\u65b9\u6cd5\u3002\u5728\u7f8e\u56fd\uff0c\u7ea6\u4e09\u5206\u4e4b\u4e8c\u7684\u4eba\u53e3\u8d85\u91cd\uff0c\u5927\u7ea6\u6709\u4e09\u5206\u4e4b\u4e00\u5219\u662f\u80a5\u80d6\uff0c\u7136\u800c\u8fd9\u4e2a\u6570\u5b57\u53ea\u4f1a\u6301\u7eed\u589e\u957f[1]<\/sup>\u3002\u80a5\u80d6\u9020\u6210\u7684\u6b7b\u4ea1\u7387\u4ec5\u6b21\u4e8e\u5438\u70df\uff0c\u9664\u6b64\u4e4b\u5916\uff0c\u7531\u4e8e\u8d85\u91cd\u548c\u80a5\u80d6\u5f15\u8d77\u7684\u5371\u9669\u56e0\u7d20\u7279\u522b\u591a\uff0c\u5305\u62ec\u7cd6\u5c3f\u75c5\uff08II\u578b\u7cd6\u5c3f\u75c5\u60a3\u8005\u4e2d80%\u662f\u80a5\u80d6\u8005\uff09\u3001\u7761\u7720\u547c\u5438\u6682\u505c\u3001\u6291\u90c1\u75c7\u3001\u9ad8\u8840\u538b\u3001\u9ad8\u8840\u8102\u548c\u9ad8\u80c6\u56fa\u9187\u7b49[2,3]<\/sup>\u3002\u56e0\u800c\u8fd9\u4e2a\u65e5\u76ca\u4e25\u91cd\u7684\u4e16\u754c\u6027\u95ee\u9898\u4e9f\u5f85\u89e3\u51b3\u3002<\/p>\n

\u8fc7\u53bb\uff0c\u4eba\u4eec\u5f80\u5f80\u901a\u8fc7\u751f\u6d3b\u65b9\u5f0f\u7684\u6539\u53d8\uff0c\u4f8b\u5982\u76d1\u6d4b\u996e\u98df\u72b6\u51b5\u6216\u8005\u953b\u70bc\u6765\u6539\u5584\u4f53\u91cd\uff0c\u4f46\u662f\u751f\u6d3b\u4e60\u60ef\u901a\u5e38\u5f88\u96be\u5728\u77ed\u671f\u5185\u6539\u53d8\uff0c\u56e0\u800c\u6548\u679c\u4e5f\u5c31\u4e0d\u660e\u663e[3]<\/sup>\u3002\u8fd9\u4e5f\u76f4\u63a5\u6216\u95f4\u63a5\u5730\u50ac\u751f\u4e86\u8bb8\u591a\u836f\u7269\u6cbb\u7597\u5242\u7684\u8bde\u751f\uff0c\u4f46\u836f\u7269\u6cbb\u7597\u9762\u4e34\u7684\u6700\u5927\u95ee\u9898\u662f\u5176\u5b89\u5168\u6027\u3002\u4e0a\u4e16\u7eaa70\u5e74\u4ee3\uff0c\u5df2\u7ecf\u6709\u90e8\u5206\u6cbb\u7597\u80a5\u80d6\u7684\u836f\u7269\u7ecfFDA\u6279\u51c6\u4e0a\u5e02\uff08\u56fe1\uff09\uff0c\u4f46\u540e\u6765\u7814\u7a76\u53d1\u73b0\u8fd9\u4e9b\u836f\u7269\u5bf9\u4eba\u4f53\u7684\u5fc3\u810f\u3001\u6d88\u5316\u7cfb\u7edf\u7b49\u9020\u6210\u8f83\u5927\u7a0b\u5ea6\u7684\u635f\u4f24\u540e\uff0c\u8fd9\u4e9b\u836f\u7269\u5c31\u7acb\u5373\u88ab\u7981\u6b62\u751f\u4ea7\u548c\u9500\u552e[2-4]<\/sup>\u3002<\/p>\n

\"\"<\/a>

\u56fe1\uff1a\u4e0a\u4e16\u7eaa70\u5e74\u4ee3\u66fe\u4e0a\u5e02\u7684\u67d0\u4e9b\u6cbb\u7597\u80a5\u80d6\u7684\u836f\u7269<\/p><\/div>\n

 <\/p>\n

\u8fd1\u5e74\u6765\uff0c\u6cbb\u7597\u80a5\u80d6\u7c7b\u836f\u7269\u7684\u7814\u7a76\u53d6\u5f97\u4e00\u4e9b\u91cd\u5927\u8fdb\u5c55\uff0c\u8d8a\u6765\u8d8a\u591a\u7684\u836f\u7269\u5f97\u5230\u6279\u51c6\u751f\u4ea7\uff0c\u5e94\u7528\u4e0a\u4e5f\u53d6\u5f97\u4e86\u4e0d\u9519\u7684\u6548\u679c\u3002\u672c\u6587\u5c06\u5bf9\u5176\u4e2d\u7684\u4e00\u79cd\u836f\u7269Lorcaserin\uff08\u4e0b\u56fe\u6240\u793a\uff09\u8fdb\u884c\u8f83\u4e3a\u8be6\u7ec6\u4ecb\u7ecd\u3002<\/p>\n

\"\"<\/a><\/p>\n

\u4e34\u5e8a\u8bd5\u9a8c\u4e2d\uff0c\u670d\u7528\u836f\u7269\u51cf\u91cd\u5e73\u5747\u7ea6\u4e3a5.5 kg\uff0c\u8fd9\u4e2a\u7ed3\u679c\u770b\u4e0a\u53bb\u5e76\u4e0d\u662f\u7279\u522b\u660e\u663e[3]<\/sup>\u3002\u53ea\u8003\u8651\u51cf\u91cd\u6570\u91cf\uff0cLorcaserin\u663e\u7136\u4e0d\u662f\u6700\u6709\u6548\u7684\u51cf\u80a5\u836f\u7269\uff0c\u4f46\u5176\u826f\u597d\u7684\u5b89\u5168\u6027\u548c\u9002\u7528\u6027\u4f7f\u5b83\u5728\u540c\u7c7b\u836f\u7269\u4e2d\u8131\u9896\u800c\u51fa\u3002\u5176\u4ed6\u51cf\u80a5\u836f\u7269\uff0c\u90fd\u6709\u4e00\u5b9a\u7684\u6f5c\u5728\u5371\u9669\u6027\u548c\u8f83\u4e3a\u660e\u663e\u7684\u526f\u4f5c\u7528\uff0c\u4f8b\u5982\u5934\u75db\u3001\u6076\u5fc3\u3001\u5934\u6655\u3001\u75b2\u52b3\u3001\u53e3\u5e72\u3001\u4fbf\u79d8\u7b49\uff0cLorcaserin\u76f8\u5bf9\u800c\u8a00\u66f4\u52a0\u6e29\u548c\uff0c\u526f\u4f5c\u7528\u5f88\u5c0f\uff0c\u56e0\u800c\u4e0a\u5e02\u540e\u5b83\u5728\u51cf\u80a5\u836f\u4e2d\u5f88\u53d7\u6b22\u8fce[5]<\/sup>\u3002<\/p>\n

 <\/p>\n

\u4e8c\u3001\u836f\u7406\u4f5c\u7528<\/h4>\n

Lorcaserin\u786e\u5207\u7684\u836f\u7406\u4f5c\u7528\u5c1a\u672a\u5b8c\u5168\u5f04\u6e05\u695a\uff0c\u4f46\u5df2\u7ecf\u786e\u5b9a\u7684\u662f\u5b83\u53ef\u6709\u6548\u5730\u4f5c\u4e3a\u4e2d\u67a25-\u7f9f\u8272\u80fa\u4e9a\u578b2C\u53d7\u4f53\u7684\u6fc0\u52a8\u5242\u3002\u76ee\u524d\u5df2\u786e\u5b9a\u670914\u79cd\u53d7\u4f53\u4e9a\u578b\u5c5e\u4e8e5-HT\u53d7\u4f53\u578b\uff0c\u800cLorcaserin\u5c31\u5c5e\u4e8e5-HT2<\/sub>\u53d7\u4f53\u578b\u7684\u6fc0\u52a8\u5242\uff0c\u5b83\u5bf95HT2C<\/sub>\u53d7\u4f53\u7684\u9009\u62e9\u6027\u9ad8\u4e8e5-HT2A<\/sub>\u548c5-HT2B<\/sub>\u53d7\u4f53\u3002\u7531\u4e8e\u5176\u4ed6\u7c7b\u578b\u7684\u53d7\u4f53\u4f1a\u5f71\u54cd\u5fc3\u810f\u74e3\u819c\uff0c\u5bf9\u4eba\u4f53\u9020\u6210\u635f\u5bb3\uff0c\u56e0\u800c\u8fd9\u79cd\u9009\u62e9\u6027\u5bf9\u4e8eLorcaserin\u7684\u5b89\u5168\u6027\u81f3\u5173\u91cd\u8981\u3002\u5f535-HT2C<\/sub>\u53d7\u4f53\u88ab\u6fc0\u6d3b\u65f6\uff0c\u53ef\u51cf\u5c11\u670d\u836f\u8005\u7684\u98df\u7269\u6444\u5165\u548c\u70ed\u91cf\u5438\u6536\uff0c\u4ece\u800c\u8fbe\u5230\u51cf\u80a5\u7684\u76ee\u7684[3,6]<\/sup>\u3002\u5728\u836f\u7269\u5e2e\u52a9\u7684\u540c\u65f6\uff0c\u5982\u679c\u80fd\u517b\u6210\u5065\u5eb7\u7684\u751f\u6d3b\u65b9\u5f0f\uff0c\u51cf\u91cd\u6548\u679c\u4f1a\u66f4\u597d\u3002<\/p>\n

 <\/p>\n

\u4e09\u3001\u5408\u6210\u8def\u7ebf<\/h4>\n

Lorcaserin\u7684\u5408\u6210\u53ef\u4ee5\u6709\u4e24\u79cd\u65b9\u6cd5\uff0c\u5176\u4e00\u662f\u5229\u7528\u5206\u5b50\u5185\u7684Heck\u53cd\u5e94\u3002\u9996\u5148\u5229\u7528\u4e09\u6c1f\u4e59\u9178\u9150\u4fdd\u62a4\u80fa\u57fa\u5f97\u5230\u5316\u5408\u72692<\/em><\/strong>\uff0c\u7898\u4ee3\u5f97\u5316\u5408\u72693<\/em><\/strong>\uff0c\u5229\u7528\u70ef\u4e19\u57fa\u6eb4\u5bf9\u80fa\u8fdb\u884c\u70c3\u57fa\u5316\uff0c\u5316\u5408\u72694<\/em><\/strong>\u52305<\/em><\/strong>\u901a\u8fc7\u5206\u5b50\u5185\u7684Heck\u53cd\u5e94\u5b8c\u6210\uff0c\u50ac\u5316\u52a0\u6c22\u8fd8\u539f\u53cc\u952e\u540e\u53bb\u4fdd\u62a4\u5373\u53ef\u5f97\u5230\u4e24\u79cd\u5bf9\u6620\u4f531:1\u7684\u6df7\u5408\u7269\u3002\u5229\u7528\u624b\u6027HPLC\u5206\u79bb\u5f97\u5230\u5355\u4e00\u6784\u578b\u7684R\u5f02\u6784\u4f53[7,8]<\/sup>\u3002\u7531\u4e8e\u73af\u5316\u524d\u4f534<\/em><\/strong>\u8f83\u6613\u5236\u5907\uff0c\u5e76\u4e14\u901a\u8fc7Heck\u53cd\u5e94\u5173\u73af\u6761\u4ef6\u8f83\u4e3a\u6e29\u548c\uff0c\u56e0\u800c\u66f4\u9002\u5408\u5728\u5b9e\u9a8c\u5ba4\u8fdb\u884c\u3002<\/p>\n

\"\"<\/a>

\u56fe2\uff1a\u5206\u5b50\u5185Heck\u53cd\u5e94\u5408\u6210Lorcaserin<\/p><\/div>\n

 <\/p>\n

\u5229\u7528Friedel-Crafts\u53cd\u5e94\u8fdb\u884c\u5408\u6210\u65f6\uff0c\u8d77\u59cb\u539f\u6599\u4e0e\u4e0a\u4e00\u8def\u7ebf\u76f8\u540c\uff0c\u9996\u5148\u901a\u8fc7-\u5364\u4ee3\u9170\u6c2f\u5bf9\u80fa\u8fdb\u884c\u9170\u57fa\u5316\u5f97\u5230\u4e2d\u95f4\u4f532<\/em><\/strong>\uff0c\u8fd9\u65f6\u6709\u4e24\u6761\u8def\u5f84\u53ef\u4f9b\u9009\u62e9\uff0c\u53ef\u4ee5\u5148\u8fd8\u539f\u7fb0\u57fa\u518d\u8fdb\u884c\u70f7\u57fa\u5316\uff0c\u4e5f\u53ef\u4ee5\u4fdd\u7559\u7fb0\u57fa\uff0c\u5173\u73af\u4e4b\u540e\u518d\u8fdb\u884c\u8fd8\u539f\u3002\u5b9e\u9a8c\u8bc1\u660e\uff0c\u7531\u5316\u5408\u72693<\/em><\/strong>\u5230\u5316\u5408\u72695<\/em><\/strong>\u7684\u8def\u5f84\u66f4\u597d[7,8]<\/sup>\u3002<\/p>\n

\"\"<\/a>

\u56fe3\uff1aFriedel-Crafts\u53cd\u5e94\u5408\u6210Lorcaserin<\/p><\/div>\n

 <\/p>\n

\u6beb\u65e0\u7591\u95ee\uff0c\u5de5\u4e1a\u751f\u4ea7\u4f1a\u9009\u62e9\u8fd9\u6761\u8def\u7ebf\uff0c\u539f\u56e0\u5c31\u5728\u4e8e\u8fd9\u6761\u8def\u7ebf\u64cd\u4f5c\u66f4\u7b80\u5355\uff0c\u5de5\u4e1a\u4e0a\u5f88\u5bb9\u6613\u8fdb\u884c\u9ad8\u6e29\u3001\u9ad8\u538b\u7b49\u5b9e\u9a8c\u5ba4\u4e2d\u96be\u4ee5\u8fdb\u884c\u7684\u6761\u4ef6\u3002\u5e76\u4e14Friedel-Crafts\u53cd\u5e94\u7684\u5e94\u7528\u5df2\u6709\u8d85\u8fc7\u4e00\u767e\u5e74\u7684\u5386\u53f2\uff0c\u5c24\u5176\u662f\u5728\u653e\u5927\u751f\u4ea7\u4e0a\uff0c\u662f\u4e00\u4e2a\u53ef\u9760\u7684\u5408\u6210\u65b9\u6cd5\u3002<\/p>\n

 <\/p>\n

\u53c2\u8003\u6587\u732e<\/h4>\n
    \n
  1. Taylor, J.; Dietrich, E.; Powell, J. Diabetes, Metab. Syndr. Obes<\/em>. 2013<\/strong>, 6, 209\u2013216.\u00a0DOI: 10.2147\/DMSO.S36276<\/li>\n
  2. Li, J. J. Anti-obesity: Orlistat (Xenical), In Contemporary Drug Synthesis<\/em>, Li, J. J.;Johnson, D. S., Eds., Wiley: Hoboken, 2004; pp 149\u2013159.\u00a0ISBN: 0-471-21480-9<\/li>\n
  3. Ryan, D.; Bray, G. Curr. Hypertens. Rep<\/em>. 2013<\/strong>, 15, 182\u2013189.\u00a0DOI:\u00a0\u00a010.1007\/s11906-013-0343-6<\/li>\n
  4. Higgins, G.; Sellers, E.; Fletcher, P. Trends in Pharm. Sci.<\/em> 2013<\/strong>, 34, 10.\u00a0DOI:\u00a010.1016\/j.tips.2013.08.001<\/li>\n
  5. Hoy, S. Adis Drug Eval<\/em>. 2013<\/strong>, 73, 463\u2013473.<\/li>\n
  6. Higgins, G.; Silenikes, L.; Lau, W.; de Lannoy, I.; Lee, D.; Izhakova, J.; Coen, K.; Le, A.; Fletcher, P. Psychopharmacol<\/em>. 2013<\/strong>, 226, 475\u2013490. \u00a0DOI:\u00a010.1007\/s00213-012-2919-2<\/li>\n
  7. Smith, B. M.; Smith, J. M.; et al. J. Med. Chem<\/em>. 2008<\/strong>, 51, 305\u2013313.\u00a0DOI:\u00a010.1021\/jm0709034<\/li>\n
  8. Smith, B. M.; Smith, J. M.; Tsai, J. H.; Schultz, J. A.; Gilson, C. A.; Estrada, S. A.;\u00a0Chen, R. R.; Park, D. M.; Prieto, E. B.; Gallardo, C. S.; et al. Bioorg. Med. Chem. Lett<\/em>. 2005<\/strong>, 15, 1467\u20131470.\u00a0DOI:10.1016\/j.bmcl.2004.12.080<\/li>\n<\/ol>\n

    \u672c\u6587\u7248\u6743\u5c5e\u4e8e\u00a0Chem-Station\u5316\u5b66\u7a7a\u95f4<\/a>\uff0c \u6b22\u8fce\u70b9\u51fb\u6309\u94ae\u5206\u4eab\uff0c\u672a\u7ecf\u8bb8\u53ef\uff0c\u8c22\u7edd\u8f6c\u8f7d\uff01<\/strong> <\/p>\n","protected":false},"excerpt":{"rendered":"\u4e00\u3001\u80cc\u666f 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\u6beb\u65e0\u7591\u95ee\uff0c\u5de5\u4e1a\u751f\u4ea7\u4f1a\u9009\u62e9\u8fd9\u6761\u8def\u7ebf\uff0c\u539f\u56e0\u5c31\u5728\u4e8e\u8fd9\u6761\u8def\u7ebf\u64cd\u4f5c\u66f4\u7b80\u5355\uff0c\u5de5\u4e1a\u4e0a\u5f88\u5bb9\u6613\u8fdb\u884c\u9ad8\u6e29\u3001\u9ad8\u538b\u7b49\u5b9e\u9a8c\u5ba4\u4e2d\u96be\u4ee5\u8fdb\u884c\u7684\u6761\u4ef6\u3002\u5e76\u4e14Friedel-Crafts\u53cd\u5e94\u7684\u5e94\u7528\u5df2\u6709\u8d85\u8fc7\u4e00\u767e\u5e74\u7684\u5386\u53f2\uff0c\u5c24\u5176\u662f\u5728\u653e\u5927\u751f\u4ea7\u4e0a\uff0c\u662f\u4e00\u4e2a\u53ef\u9760\u7684\u5408\u6210\u65b9\u6cd5\u3002   \u53c2\u8003\u6587\u732e Taylor, J.; Dietrich, E.; Powell, J. Diabetes, Metab. Syndr. Obes. 2013, 6, 209\u2013216.\u00a0DOI: 10.2147\/DMSO.S36276 Li, J. J. Anti-obesity: Orlistat (Xenical), In Contemporary Drug Synthesis, Li, J. J.;Johnson, D. S., Eds., Wiley: Hoboken, 2004; pp 149\u2013159.\u00a0ISBN: 0-471-21480-9 Ryan, D.; Bray, G. Curr. Hypertens. Rep. 2013, 15, 182\u2013189.\u00a0DOI:\u00a0\u00a010.1007\/s11906-013-0343-6 Higgins, G.; Sellers, E.; Fletcher, P. Trends in Pharm. Sci. 2013, 34, 10.\u00a0DOI:\u00a010.1016\/j.tips.2013.08.001 Hoy, S. Adis Drug Eval. 2013, 73, 463\u2013473. Higgins, G.; Silenikes, L.; Lau, W.; de Lannoy, I.; Lee, D.; Izhakova, J.; Coen, K.; Le, A.; Fletcher, P. 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