On February 15, 2022, Dichiara, Maria; Artacho-Cordon, Antonia; Turnaturi, Rita; Santos-Caballero, Miriam; Gonzalez-Cano, Rafael; Pasquinucci, Lorella; Barbaraci, Carla; Rodriguez-Gomez, Isabel; Gomez-Guzman, Manuel; Marrazzo, Agostino; Cobos, Enrique J.; Amata, Emanuele published an article.Category: piperidines The title of the article was Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation. And the article contained the following:
The development of σ1 receptor antagonists hybridized with a H2S-donor is here reported. We aimed to obtain improved analgesic effects when compared to σ1 receptor antagonists or H2S-donors alone. In an in vivo model of sensory hypersensitivity, thioamide 1a induced analgesia which was synergistically enhanced when associated with the σ1 receptor antagonist BD-1063. The selective σ1 receptor agonist PRE-084 completely reversed this effect. Four thioamide H2S-σ1 receptor hybrids (5a-8a) and their amide derivatives (5b-8b) were synthesized. Compound 7a (AD164) robustly released H2S and showed selectivity for σ1 receptor over σ2 and opioid receptors. This compound induced marked analgesia that was reversed by PRE-084. The amide analog 7b (AD163) showed only minimal analgesia. Further studies showed that 7a exhibited negligible acute toxicity, together with a favorable pharmacokinetic profile. To the best of our knowledge, compound 7a is the first dual-acting ligand with simultaneous H2S-release and σ1 antagonistic activities. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Category: piperidines
The Article related to pain analgesic effect pharmacokinetics antagonism, analgesia, antagonist, dual ligands, hydrogen sulfide donor, sigma-1 receptor, Placeholder for records without volume info and other aspects.Category: piperidines
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Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem