Animal studies suggest that the transient receptor potential ion channels TRPM8 and TRPA1 are cold sensors and that sodium channels Nav1.8 and Nav1.7 are essential for detecting pain induced by cold temperatures. This study aims to validate these findings in humans.

开始日期2023-07-07

申办/合作机构

Medical University of Vienna

NCT01812265 / Completed临床1期

A Double Blind (3rd Party Open), Randomized, Placebo Controlled, Crossover Study To Investigate The Effects Of Pf-06305591 On Cold Pain In Healthy Male Subjects

This study will evaluate the pharmacological activity of PF-06305591 in healthy male volunteers by assessing the effects of two dose levels of PF-06305591 on cold pain intensity evoked by keeping non-dominant hand into a water bath kept at 2+/- degrees.

开始日期2013-06-01

申办/合作机构

Pfizer Inc.

NCT01776619 / Completed临床1期

A Double Blind (3rd Party Open) Randomized, Dose Escalation Study to Investigate the Safety, Tolerability, Pharmacokinetics of Repeat Doses PF-06305591 Combined With a Cross-over Relative Bioavailability and Food Effect Evaluation After Single Dose of PF-06305591 in Healthy Young Subjects

Safety, tolerability and PK of repeated doses of PF-06305591 will be evaluated in young healthy volunteers toghether with food effect on relative bioavailability of solid formulation after single dose.

开始日期2013-04-01

申办/合作机构

Pfizer Inc.

100 项与 PF-6305591 相关的临床结果

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100 项与 PF-6305591 相关的转化医学

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100 项与 PF-6305591 相关的专利（医药）

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项与 PF-6305591 相关的文献（医药）

2019-01-01·Bioorganic & medicinal chemistry3区 · 医学

The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain

3区 · 医学

Article

作者: Murata, Yoshihisa ; Blackwell, Paul ; Warmus, Joseph S ; Miller, Duncan ; Brown, Bruce ; Stevens, Edward B ; Blakemore, David C ; Bagal, Sharan K ; Klute, Wolfgang ; Malet Sanz, Laia ; Gray, Victoria ; Skerratt, Sarah ; Brown, Alan D ; Kemp, Mark ; Fengas, David ; Fenwick, David R ; Crawforth, James ; Payne, C Elizabeth ; Bungay, Peter J ; Corless, Martin

The voltage gated sodium channel Na_V1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole Na_V1.8 blockers. Subsequent optimization allowed the identification of compound 9, PF-06305591, as a potent, highly selective blocker with an excellent preclinical in vitro ADME and safety profile.

100 项与 PF-6305591 相关的药物交易

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