Dacemazine Explained

Dacemazine (INN, also known as Ahistan and Histantine)[1] is a phenothiazine derivative which acts as a histamine antagonist at the H1 subtype. First described in 1951, it was never marketed as a drug on its own, although a combination of dacemazine and di-tert-butylnaphthalenesulfonate was sold as an antispasmodic and antitussive under the trade name Codopectyl.[1] It was also assessed as a possible anticancer drug.[2]

Synthesis

Amide formation between phenothiazine (1) and chloroacetyl chloride (2) gives 10-(Chloroacetyl)-phenothiazine [786-50-5] (3). The subsequent displacement of the remaining halogen with dimethylamine (4) completes the synthesis of dacemazine (5).

Notes and References

  1. Book: Triggle DJ, Ganellin CR, MacDonald F . Dictionary of Pharmacological Agents . Chapman & Hall/CRC . Boca Raton . 1996 . 1 . 711 . 0-412-46630-9 . Retrieved on August 2, 2008 through Google Book Search.
  2. Karolyhazy G, Havas I, Jansco G, Kapas L, Sellei C . [The anticarcinogenic effect of dimethylaminoacetyl-phentiazide (ahistan)] . ro . Kiserletes Orvostudomany . 4 . 4 . 260–2 . August 1952 . 13023855 .