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Salvinorin B mesylate (Mesyl Sal B) is a selective κ-opioid receptor agonist that is more potent than salvinorin A (Item No. 11487) in CHO cells transfected with the human κ-opioid receptor (EC50s = 30 and 40 nM, respectively).1,2 It is a mesylated version of salvinorin B (Item No. 11488) and is highly selective for κ-opioid receptors over µ- and δ-opioid receptors.1 In vitro, it increases dopamine uptake via the dopamine transporter (DAT) in an ERK1/2-dependent manner but does not alter expression of DAT on the cell membrane.3 In rats, it increases the pain threshold and blocks reinstatement of cocaine drug-seeking.
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1. Neoclerodane diterpenes as a novel scaffold for μ opioid receptor ligands. J. Med. Chem. 48(15), 4765-4771 (2005).
2. Synthesis of salvinorin A analogues as opioid receptor probes. J. Nat. Prod. 69, 914-918 (2006).
3. Pharmacology and anti-