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AMPA¨üÅé¼W®Ä¾¯TAK-137§@¬°ºë¯«¤Àµõ¯gªvÀøÃĪ«ªºÁ{§É«e¯S¼x
www.ncbi.nlm.nih.gov/pmc/articles/PMC6507438/
³ø§i¤º®e¤jP¬° ( google ½Ķ )
. ºë¯«¤Àµõ¯g¬O¤@ºØºC©Êºë¯«¯e¯f¡A¨ã¦³¤@¨t¦C¯gª¬¡G¶§©Ê¡A³±©Ê©M»{ª¾¯gª¬¡C¤w¸g°ò©óÁ{§Éµo²{«ü¥X¤Fºë¯«¤Àµõ¯gªº¯f²z¥Í²z¾ÇªºY¤z°²³]¡C°ª«×¦h¤ÚÓi°²»¡³Q»{¬°¬O¶§©Ê¯gª¬ªº¥Dnì¦]¡A¨Ã¥B§C¨¦®ò»Ä°²»¡¤£¶È°w¹ï¶§©Ê¯gª¬¦Ó¥B°w¹ï®ø·¥©M»{ª¾¯gª¬´£¥X
. ¨¦®ò»Ä¨t²Îªº¤U½Õ¥i¯à¯A¤Îºë¯«¤Àµõ¯gªº¶§©Ê¡A³±©Ê©M»{ª¾¯gª¬¡C³q¹L¼W±jªº¨¦®ò»Ä«H¸¹¶Ç¾É¡AAMPA¨üÅé¡]¤@ºØÂ÷¤l«¬¨¦®ò»Ä¨üÅé¡^ªº¬¡¤Æ¥i¯à¬Oºë¯«¤Àµõ¯gªº¤@ºØ·sªºªvÀøµ¦²¤¡CTAK -137¬O¤@ºØ¨ã¦³³Ì¤p¿E°Ê¬¡©Êªº·s«¬AMPA¨üÅé¼W®Ä¾¯; ¦b³o¶µ¬ã¨s¤¤¡A§Ų́ϥÎø¥¾¦°Êª«©M«D¤HÆFªøÃþ°Êª«¨Óµû¦ô¨ä§@¬°ºë¯«¤Àµõ¯gÃĪ«ªº¼ç¤O¡C
. AMPA¨üÅ骺¿E¬¡¾ÉPNMDA¨üÅé¥\¯à¼W¥[; ¦]¦¹¡AAMPA¨üÅé¼W®Ä¾¯¨ã¦³§@¬°ºë¯«¤Àµõ¯gªºªvÀøÃĪ«ªº¼ç¤O¡CµM¦Ó¡A¥ý«e³ø¾Éªº¤Æ¦Xª«¤w¸gªí©ú¤F½Ñ¦pÄÁ§Î¤ÏÀ³©M»¤µoÅöíwµo§@µ¥·ÀI¡CLY451646©MLY404187ªºÅ餺¬ã¨sÅã¥Ü¨ä°~®kªºÄÁ§ÎÅTÀ³¡C§Ú̳̪ñµo²{¤F¤@ºØ·s«¬AMPA¨üÅé¼W®Ä¾¯-TAK-137¡]9-¡]4-f®ñ°òf°ò¡^-3,4-¤G²BýmÔr¨Ã[2,1-c] [1,2,4]噻¤G嗪2,2-¤G®ñ¤Æª«¡^¡A¥Ñ©ó¨ä§C¿E°Ê¬¡©Ê¡A°§C¤FÄÁ§Î¾¯¶q¤ÏÀ³©MÅöíwµo§@ªº·ÀI¡C
. ¼Æ¾Úªí©ú¡A¨ã¦³§C¤º¦b¬¡©ÊªºTAK-137«¬AMPA¨üÅé¼W®Ä¾¯¥i¯à¬OªvÀøºë¯«¤Àµõ¯g¦hºØ¯gª¬ªº¦³§Æ±æªºªvÀø¤èªk¡A¤×¨ä¬O¹ï©ó®ø·¥©M»{ª¾¯gª¬¡C
. TAK‐137 significantly inhibited METH‐induced hyperlocomotion in rats to 33.6 ¡Ó 7.66% of that in the control ; §í¨î¦Ê¤À¤ñ§C©ó§Üºë¯«¯fÃĪ«¡A¨ä¦bD2R¦û¾Ú60¢H®Éªí²{¥X¤j©ó50¢Hªº§í¨î§@¥Î¡C¦]¦¹TAK-137¥i¥H¨ã¦³¦³ªº¹ïºë¯«¤Àµõ¯gªº¶§©Ê¯gª¬ªº¥\®Ä¡C»P³ø¾Éªº¨ã¦³¦h¤ÚÓiD2«ú§Ü§@¥Îªº§Üºë¯«¯fÃĤ£¦P¡ATAK-137¤£·|»¤¾ÉÅãµÛªº»ø¦í¤ÏÀ³©M¦å¼ß¤¤¶Ê¨Å¯À©M¸²µå¿}¤ô¥ªº¼W¥[.
. ¥Ø«eªº§Üºë¯«¯fÃīܤ֯à§ïµ½³±©Ê¯gª¬¡CTAK-137¨ã¦³§ïµ½»PNMDA¨üÅé¥\¯à´î°h¬ÛÃöªºªÀ·|¦æ¬°ªº¼ç¤O¡C
. TAK-137¹ï»{ª¾¯gª¬¡A¯S§O¬Oª`·N¤O¡A¤u§@°O¾Ð©M°õ¦æ±±¨îªº¼vÅT¡A¦]¬°³o¨Ç³Q»{¬°¬Oºë¯«¤Àµõ¯g¤¤¨ü·lªºÃöÁä»{ª¾»â°ì¡A³q¹L§ïµ½ºë¯«¤Àµõ¯g¤¤ªº»{ª¾ªº´ú¶q©MªvÀø¬ã¨s¡C
. TAK-137ªº¯S¼x¦b©ó°w¹ï®ø·¥©M»{ª¾¯gª¬ªº¯S©w¥\®Ä¡C¦]¦¹¡A§Ú̬ã¨s¤F¦P®É¨Ï¥ÎTAK-137©M§Üºë¯«¯fÃĪ«ªº¼vÅT¡CTAK-137¤£·|¤zÂZ¶ø´á¥¹ïMETH»¤¾Éªº¹L«×¹B°Êªº¼vÅT¡A¨Ã¥B¤£·|¥[¼@»ø¦í¤ÏÀ³©M¦å¼ß¶Ê¨Å¯À¤ô¥¡C¦¹¥~¡A¶ø´á¥ªºÁp¦XªvÀø¨Ã¥¼§ïÅÜTAK-137¹ï»{ª¾ªº¼vÅT¡C¦]¦¹¡ATAK-137»P¥Ø«e¥i¥Îªº§Üºë¯«¯fÃĪº²Õ¦X¥i¦³¯q©óªvÀøºë¯«¤Àµõ¯gªº¦hºØ¯gª¬¡C¦b¸Ó¬ã¨s¤¤¥¼ÀË´ú¨ì¥\®Äªº¨ó¦P¼W±j¡A³o¥i¯à¬O¶ø´á¥¹ïD2R«ú§Ü§@¥Îªº¤£¦P§@¥Î¾÷¨î©MTAK-137¹ï¨¦®ò»Ä«H¸¹ªº¼W±j§@¥Îªºµ²ªG¡C
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¦ý¬OTAK-137«o¹L¤£¤F phase 1 ªºÃö¥d , ³QªZ¥Ð¤¤(²×)¤î¬ãµo¤F
clinicaltrials.gov/ct2/results?cond=&term=Tak-137&cntry=&state=&city=&dist=
www.pharmacodia.com/yaodu/html/v1/chemicals/6605cf6f932aa6510d637af51c820a6a.html
TAK-137 was developed by Takeda for the treatment of attention deficit hyperactivity disorder, neurological and psychiatric disorders.
Pharmacokinetic variability has led to a decrease in the compound¡¦s safety margin. So Takeda discontinued this studies in 2015.
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en.wikipedia.org/wiki/Breakthrough_therapy
If the designation is no longer supported by subsequent data, FDA may rescind the designation.
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en.wikipedia.org/wiki/Breakthrough_therapy
If the designation is no longer supported by subsequent data, FDA may rescind the designation.
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en.wikipedia.org/wiki/Breakthrough_therapy
Drugs that have been granted breakthrough status are given priority review. The FDA works with the sponsor of the drug application to expedite the approval process. This expedited process can include rolling reviews, smaller clinical trials, and alternative trial designs.
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health.udn.com/health/story/10561/3833934
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JNJ ªº Spravato ªºµP»ù(?) (ÁÙ¬O³o»ò¶Q?)
Known as esketamine and marketed as Spravato, the nasal spray was developed by Johnson & Johnson (JNJ).
The initial month of therapy can cost from $4,720 to $6,785, while subsequent treatment can cost $2,360 to $3,540.
The annual tab might run from $33,000 to about $49,200.
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