Abstract
1-(Benzothiazol-2-yl)-1-(4-chlorophenyl)ethanol (1) was identified as a positive allosteric modulator (PAM) of the CaSR in a functional cell-based assay. This compound belongs to a class of compounds that is structurally distinct from other known positive allosteric modulators, for example, the phenylalkylamines cinacalcet, a modified analog (13) potently suppressed parathyroid hormone (PTH) release in rats, consistent with its profile as a PAM of CaSRs.
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MeSH terms
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Allosteric Regulation
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Animals
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Benzothiazoles / chemical synthesis
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Benzothiazoles / chemistry*
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Benzothiazoles / pharmacology
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Benzyl Alcohols / chemistry*
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Benzyl Alcohols / pharmacology
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Cinacalcet
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Drug Evaluation, Preclinical
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Humans
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Microsomes, Liver / metabolism
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Naphthalenes / chemistry
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Parathyroid Hormone / metabolism
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Phenylethyl Alcohol / chemical synthesis
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Phenylethyl Alcohol / chemistry*
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Phenylethyl Alcohol / pharmacology
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Rats
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Receptors, Calcium-Sensing / chemistry*
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Receptors, Calcium-Sensing / metabolism
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Structure-Activity Relationship
Substances
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Benzothiazoles
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Benzyl Alcohols
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Naphthalenes
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Parathyroid Hormone
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Receptors, Calcium-Sensing
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Phenylethyl Alcohol
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Cinacalcet