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https://t.co/l03ezVUu0g "which were at lower concentrations a H1R antagonist but at higher concentrations in an H2R antagonist (Klein and Levey 1971)."
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https://t.co/l03ezVUu0g "Because these early researchers had no H2R antagonist at their disposal, they could only block the activity of adenylyl cyclases with very high concentrations of promethazine,"
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https://t.co/l03ezVUu0g "Further studies on mutations revealed that G-protein coupled receptor kinase 2 and 3 (GRK2 and GRK3) in COS-7 cells (a fibroblast-like cell line) led to the desensitisation of H2R in histamine (Rodriguez-Pena et al., 2000)."