Congener derivatives and conjugates of histamine: synthesis and tissue and receptor selectivity of the derivatives.

摘要: A series of 19 congener derivatives and conjugates histamine was synthesized tested to determine whether the ligands would alter conventional activity in various tissues. The derivatives, which contained either branched or unbranched aliphatic groups, aromatic amide dipeptides, exhibited affinities for type 1 and/or 2 receptors that were widely different from progenitor. p-trifluoromethyl derivative with an intermediate chain length four methylenes (compound 13) most potent lymphocytes H2 receptor agonist but inactive on guinea pig myocardium receptors. deletion a single methylene 12) this compound resulted total loss its H1 aorta. Compound 12 became exclusive dipeptide conjugate 17) 18), both methylenes, retained some receptors, lost their Therefore, can be modified at sites are distance imidazole moiety, resulting tissue selective agonists.