Abstract
The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and have the potential as an oral, anabolic treatment for osteoporosis.
MeSH terms
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Administration, Oral
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Allosteric Regulation / drug effects*
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Anabolic Agents
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Animals
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Cell Line
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Cyclopropanes / chemistry*
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Cyclopropanes / pharmacokinetics
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Cyclopropanes / pharmacology
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Drug Discovery
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Humans
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Indans / chemistry*
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Indans / pharmacokinetics
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Indans / pharmacology
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Microsomes, Liver
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Osteoporosis / drug therapy
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Phenylpropionates / chemistry*
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Phenylpropionates / pharmacokinetics
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Phenylpropionates / pharmacology
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Rats
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Receptors, Calcium-Sensing / antagonists & inhibitors*
Substances
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Anabolic Agents
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Cyclopropanes
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Indans
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Phenylpropionates
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Receptors, Calcium-Sensing
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cyclopropanecarboxylic acid
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ronacaleret