Abstract
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists with greater selectivity over hERG were identified. SAR studies addressing two distinct alternatives for structural modifications leading to improve hERG selectivity are described.
MeSH terms
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Biphenyl Compounds / chemical synthesis
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Biphenyl Compounds / pharmacology*
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ERG1 Potassium Channel
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Ergolines / pharmacology
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Ether-A-Go-Go Potassium Channels / drug effects*
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Humans
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Indicators and Reagents
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Mianserin / pharmacology
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Naphthalenes / chemical synthesis
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Naphthalenes / pharmacology*
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Potassium Channel Blockers / pharmacology*
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Receptor, Serotonin, 5-HT2C / drug effects
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Receptors, Somatostatin / antagonists & inhibitors*
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Serotonin Antagonists / pharmacology
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Structure-Activity Relationship
Substances
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Biphenyl Compounds
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ERG1 Potassium Channel
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Ergolines
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Ether-A-Go-Go Potassium Channels
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Indicators and Reagents
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KCNH2 protein, human
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MCHR1 protein, human
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Naphthalenes
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Potassium Channel Blockers
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Receptor, Serotonin, 5-HT2C
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Receptors, Somatostatin
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Serotonin Antagonists
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aminomethyl tetrahydronaphthalene biphenyl carboxamide
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Mianserin
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mesulergine