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10.1021/ml100268k http://scihub22266oqcxt.onion/10.1021/ml100268k C4018071!4018071 !24900301     free     free     free Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\24900301 .jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       ACS+Med+Chem+Lett 2011 ; 2 (3 ): 238-42 Nephropedia Template TP {{tp|p=24900301 |t=2011. Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone |pdf=|usr=}}{{24900301 }} gab.com Text Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900301 #FOAvip Short-acting oral calcilytics, calcium-sensing receptor (CaSR) antagonists, have been considered as alternatives for parathyroid hormone (PTH), an injectable bone anabolic drug used in the treatment of osteoporosis. Previously, we identified aminopropandiol 1, which transiently stimulated endogenous PTH secretion in rats. However, the inhibition of cytochrome P450 (CYP) 2D6 and the low bioavailability of 1 remain to be solved. Attempts to change the physicochemical properties of the highly lipophilic amine 1 by introduction of a carboxylic acid group as well as further structural modifications led to the discovery of the highly potent biphenylcarboxylic acid 15, with a markedly reduced CYP2D6 inhibition and a significantly improved bioavailability. Compound 15 evoked a rapid and transient elevation of endogenous PTH levels in rats after oral administration in a dose-dependent manner at a dose as low as 1 mg/kg. The PTH secretion pattern correlated with the pharmacokinetic profile and agreed well with that of the exogenous PTH injection which exerts a bone anabolic effect. Twit Text FOAVip Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900301 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24900301 #FOAvip English Wikipedia <ref>{{Cite pmid|24900301 }}</ref> Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone #MMPMID24900301 Shinagawa Y ; Inoue T ; Katsushima T ; Kiguchi T ; Ikenogami T ; Ogawa N ; Fukuda K ; Hirata K ; Harada K ; Takagi M ; Nakagawa T ; Kimura S ; Matsuo Y ; Maekawa M ; Hayashi M ; Soejima Y ; Takahashi M ; Shindo M ; Hashimoto H ACS Med Chem Lett 2011[Mar]; 2 (3 ): 238-42 PMID24900301 show ga Short-acting oral calcilytics, calcium-sensing receptor (CaSR) antagonists, have been considered as alternatives for parathyroid hormone (PTH), an injectable bone anabolic drug used in the treatment of osteoporosis. Previously, we identified aminopropandiol 1, which transiently stimulated endogenous PTH secretion in rats. However, the inhibition of cytochrome P450 (CYP) 2D6 and the low bioavailability of 1 remain to be solved. Attempts to change the physicochemical properties of the highly lipophilic amine 1 by introduction of a carboxylic acid group as well as further structural modifications led to the discovery of the highly potent biphenylcarboxylic acid 15, with a markedly reduced CYP2D6 inhibition and a significantly improved bioavailability. Compound 15 evoked a rapid and transient elevation of endogenous PTH levels in rats after oral administration in a dose-dependent manner at a dose as low as 1 mg/kg. The PTH secretion pattern correlated with the pharmacokinetic profile and agreed well with that of the exogenous PTH injection which exerts a bone anabolic effect. äDiscovery of a potent and short-acting oral calcilytic with a pulsatil(epmc).pdf DeepDyve Pubget Overpricing