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2Â¥2012-10-23 19:43:46
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ÊÇÒòΪ¿´µ½Ò»´ó¶ÎµÄÓ¢ÎĶøÃ»ÈË»ØÃ´£¿ Çë¾Í¿´Õâ3¾ä£º »¯ºÏÎï17¡¢29µÄ Modification of the amino substituent gave the isomeric tetramethyl derivative 17 and the 4,7-dihydroindanyl indacaterol derivative 29 which had comparable decreases in affinity and selectivity when compared to 1. »¯ºÏÎï16µÄ Introduction of the a-methyl group into the amino substituent gave the analogue 25 which led to the anticipated increase in b2adrenoceptor affinity, of greater than 10-fold relative to 1.However, this increase in affinity was also accompanied by an even greater relative increase in b1-adrenoceptor affinity and an overall reduction in binding selectivity. лл£¡£¡£¡ |
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