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Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.

ABSTRACT: Neuronal nicotinic receptors have been implicated in several diseases and disorders such as autism, Alzheimer's disease, Parkinson's disease, epilepsy, and various forms of addiction. To understand the role of nicotinic receptors in these conditions, it would be beneficial to have selective molecules that target specific nicotinic receptors in vitro and in vivo. Our laboratory has previously identified novel negative allosteric modulators of human ?4?2 (H?4?2) and human ?3?4 (H?3?4) nicotinic receptors. The effects of novel sulfonylpiperazine analogues that act as negative allosteric modulators on both H?4?2 nAChRs and H?3?4 nAChRs were investigated. This work, through structure-activity relationship (SAR) studies, describes the chemical features of these molecules that are important for both potency and selectivity on H?4?2 nAChRs.

SUBMITTER: Henderson BJ

PROVIDER: S-EPMC3240716 | biostudies-literature | 2011 Dec

REPOSITORIES: biostudies-literature

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Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.

Henderson Brandon J BJ Carper Daniel J DJ González-Cestari Tatiana F TF Yi Bitna B Mahasenan Kiran K Pavlovicz Ryan E RE Dalefield Martin L ML Coleman Robert S RS Li Chenglong C McKay Dennis B DB

Journal of medicinal chemistry 20111118 24

Neuronal nicotinic receptors have been implicated in several diseases and disorders such as autism, Alzheimer's disease, Parkinson's disease, epilepsy, and various forms of addiction. To understand the role of nicotinic receptors in these conditions, it would be beneficial to have selective molecules that target specific nicotinic receptors in vitro and in vivo. Our laboratory has previously identified novel negative allosteric modulators of human α4β2 (Hα4β2) and human α3β4 (Hα3β4) nicotinic re ...[more]

PMID: 22060139

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Dataset Information

Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.

Publications

Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.

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