Anti-histamine

Classical Receptor Antagonists. Since the initial discovery of an anti-histaminic compound in 1933, a very high number of potent compounds were... 

More typical examples are the amino ethers (3) used as anti-histamine or anti-Parkinson drugs according to the substituents. These are obviously derived from the alcohols (4) which are made from an aryl Grignard reagent and a benzaldehyde. Either starting material may bear the substituent X the choice can be made according to availability and so that side reactions are avoided,... 

Suggest a synthesis for (38), needed for trial as an anti-histamine,... 

Suggest a synthesis for (19), needed in the search for new anti-histamines. 

Azanator (59) represents a more classical anti-histaminic structure, since the more basic nitrogen in this case occurs in the side chain. Preparation... 

Histamine receptors on parietal cells belong to the H2 type (p. 114) and are blocked by H2-antihistaniines. Because histamine plays a pivotal role in the activation of parietal cells, H2-anti-histamines also diminish responsivity to other stimulants, e.g gastrin (in gas-2000 Thieme... 

Chang AB, Peake J, McElrea MS. Anti-histamines for prolonged non-specific cough in children. Cochrane Database Syst Rev 2006. 

J. P. Desager, Y. Horsmans (1995). Pharmacokinetic-pharmacodynamic relationships of Hl-anti-histamines. Clin. Pharmacokinet. 28 418. 

Cafieri F, Fattorusso E, Mangoni A, Taglialatela-Scafati O (1996) Dispacamides, Anti-Histamine Alkaloids from Caribbean Agelas Sponges. Tetrahedron Lett 37 3587... 

Cafieri F, Camuccio R, Fattorusso E, Taglialatela-Scafati O, Vallefuoco T (1997) Anti-Histaminic Activity of Bromopyrrole Alkaloids Isolated from Caribbean Agelas Sponges. Bioorg Med Chem Lett 7 2283... 

Ciminiello P, Dell Aversano C, Fattorusso E, Magno S (2001) Archerine, a Novel Anti-Histaminic Bromotyrosine-Derived Compound from the Caribbean Marine Sponge Aplysina archeri. Eur J Org Chem 55... 

During the Second World War, Union Chimique Beige started producing basic pharmaceuticals such as calcium, phosphor, vitamins, insulin, and sulfamides. However, it was only in the late fifties that it launched, with limited market impact, its first real pharmaceutical products - Postafene (an anti-histamine), Atarax (a tranquilizer) and Tuclase (a cough and cold drug) - and concluded a first license agreement with Pfizer for the distribution of Atarax in the U.S. 

Other than protein, histamine in human blood samples was determined by the immunoassay method. It was detected by its binding with anti-histamine IgG, which was coupled to ferrocene (Fc-IgG). Separation of histamine and its complex with antibody was based on p/ differences, and it was achieved in a PMMA chip consisting of a multichannel matrix column coated with a cation-exchange resin (Nation). Histamine was detected electrochemically a decrease in the current due to Fc-IgG occurred after its binding to histamine [1012],... 

Pruritus of the elderly is another common dermatosis associated with itch.5 One study has shown that elderly patients with generalized pruritus had a higher degree of skin dryness than in age matched control subjects.6 This study also demonstrated that skin surface conductance, a marker of stratum corneum water content, was decreased in elderly patients with generalized pruritus. The study was also successful in demonstrating an acquired abnormality in keratinization in these patients. This abnormality manifested with increased intracorneal cohesion compared with the controls. Another study showed an increase in histamine release and hypersensitivity in patients with senile pruritus.7 Paradoxically, oral anti-histamines are not very efficacious in the treatment of senile pruritus. 

Quinones, C., Caceres, J., Stud, M., and Martinez, A., Prediction of drug half-life values of anti-histamines based on the CODES/neural network model, Quant. Struct.-Act. Relat., 19, 448 -54, 2000. 

Dale HH. Foreword. In Handbook of Exp. Pharmacol. XVIII-1, Histamine and anti-Histamines. Rocha e Silva M (Ed.) Springer-Verlag, Berlin, 1966. 

The treatments for allergies try to lessen their effects by using anti-histamine... 

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