Lack of Detection of the Analgesic Properties of PF-05089771, a Selective Nav1.7 Inhibitor, Using a Battery of Pain Models in Healthy Subjects was written by Siebenga, Pieter;van Amerongen, Guido;Hay, Justin L.;McDonnell, Aoibhinn;Gorman, Donal;Butt, Richard;Groeneveld, Geert Jan. And the article was included in Clinical and Translational Science in 2020.Computed Properties of C18H12Cl2FN5O3S2 This article mentions the following:
The aim was to demonstrate analgesic properties of a potent selective Nav1.7 sodium channel blocker, PF-05089771, alone and concomitantly with pregabalin in healthy subjects using a battery of human evoked pain models. This was a double-blind, double-dummy, randomized, placebo-controlled, five-period cross-over study with PF-05089771 alone and PF-05089771 concomitantly with pregabalin as treatment arms with pregabalin, ibuprofen, and placebo as control arms (NCT02349607). A battery of human evoked pain models was used to investigate analgesic properties of PF-05089771. Twenty-five subjects were enrolled in the study of which 23 subjects completed all five periods. PF-05089771 alone did not differ from placebo on the primary pain end points. The same holds when comparing PF-05089771 concomitantly with pregabalin and pregabalin alone. Pregabalin showed significant effects relative to placebo on thermal pain on the normal skin and UVB skin (least squares means with 90% confidence interval: 0.63 (0.32-0.93) and 0.53 (0.11-0.96)), pressure stimulation (1.10 (1.04-1.18)), and cold pressor (1.22 (1.14-1.32)). Ibuprofen demonstrated significant effects on thermal pain UVB skin (1.26 (0.82-1.70)) and pressure stimulation assessment (1.08 (1.01-1.15)), consistent with historical results. This study did not demonstrate analgesic properties of PF-05089771 alone or concomitantly with pregabalin in a battery of pain models. In the experiment, the researchers used many compounds, for example, 4-(2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide (cas: 1235403-62-9Computed Properties of C18H12Cl2FN5O3S2).
4-(2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide (cas: 1235403-62-9) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Computed Properties of C18H12Cl2FN5O3S2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica