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View article: Tebuconazole bioconcentration in European Eels (Anguilla Anguilla): the role of pollutant cocktails
Tebuconazole bioconcentration in European Eels (Anguilla Anguilla): the role of pollutant cocktails Open
European eel (Anguilla anguilla) populations are in decline across Europe, with organic pollutants (OPs) identified as one of the contributing factors. In the Albufera of Valencia, a critical feeding and maturation habitat for this species…
View article: Phenylalanine-derived β-lactam TRPM8 antagonists: revisiting configuration and new benzoyl derivatives
Phenylalanine-derived β-lactam TRPM8 antagonists: revisiting configuration and new benzoyl derivatives Open
Aim: To expand the understanding of the structure-activity relationship within a family of amino acid-derived β-lactam TRPM8 (transient receptor potential melastatin channel, subtype 8) antagonists, this work investigated both the configur…
View article: β-Lactam TRPM8 Antagonists Derived from Phe-Phenylalaninol Conjugates: Structure–Activity Relationships and Antiallodynic Activity
β-Lactam TRPM8 Antagonists Derived from Phe-Phenylalaninol Conjugates: Structure–Activity Relationships and Antiallodynic Activity Open
The protein transient receptor potential melastatin type 8 (TRPM8), a non-selective, calcium (Ca2+)-permeable ion channel is implicated in several pathological conditions, including neuropathic pain states. In our previous research endeavo…
View article: β-Lactam TRPM8 Antagonists Derived from Phe-Penylalaninol Conjugates: Structure-Activity Relationships and Antiallodynic Activity
β-Lactam TRPM8 Antagonists Derived from Phe-Penylalaninol Conjugates: Structure-Activity Relationships and Antiallodynic Activity Open
The protein TRPM8, a non-selective, calcium (Ca2+) permeable ion channel is implicated in several pathological conditions, including neuropathic pain states. In our previous research endeavors, we have identified β–lactam derivatives with …
View article: New TRPM8 blockers exert anticancer activity over castration-resistant prostate cancer models
New TRPM8 blockers exert anticancer activity over castration-resistant prostate cancer models Open
View article: β–Lactam TRPM8 Antagonist RGM8-51 Displays Antinociceptive Activity in Different Animal Models
β–Lactam TRPM8 Antagonist RGM8-51 Displays Antinociceptive Activity in Different Animal Models Open
Transient receptor potential melastatin subtype 8 (TRPM8) is a cation channel extensively expressed in sensory neurons and implicated in different painful states. However, the effectiveness of TRPM8 modulators for pain relief is still a ma…
View article: In Vitro and In Vivo Pharmacological Characterization of a Novel TRPM8 Inhibitor Chemotype Identified by Small-Scale Preclinical Screening
In Vitro and In Vivo Pharmacological Characterization of a Novel TRPM8 Inhibitor Chemotype Identified by Small-Scale Preclinical Screening Open
Transient receptor potential melastatin type 8 (TRPM8) is a target for the treatment of different physio-pathological processes. While TRPM8 antagonists are reported as potential drugs for pain, cancer, and inflammation, to date only a lim…
View article: New TRPM8 Blockers Exert Anticancer Activity Over Castration-Resistant Prostate Cancer Models
New TRPM8 Blockers Exert Anticancer Activity Over Castration-Resistant Prostate Cancer Models Open
View article: Phenylalanine-Derived β-Lactam TRPM8 Modulators. Configuration Effect on the Antagonist Activity
Phenylalanine-Derived β-Lactam TRPM8 Modulators. Configuration Effect on the Antagonist Activity Open
Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a Ca2+ non-selective ion channel implicated in a variety of pathological conditions, including cancer, inflammatory and neuropathic pain. In previous works we iden…
View article: Highly functionalized β-lactams and 2-ketopiperazines as TRPM8 antagonists with antiallodynic activity
Highly functionalized β-lactams and 2-ketopiperazines as TRPM8 antagonists with antiallodynic activity Open
View article: Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities
Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities Open
[Image: see text] Transient receptor potential melastatin 8 (TRPM8) ion channel represents a valuable pharmacological option for several therapeutic areas. Here, a series of conformationally restricted derivatives of the previously describ…