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We determined the molecular properties of the selective and potent H1-receptor agonist histaprodifen and its N substituted analogues: methyl-, dimethyl-, and imidazolylethyl-histaprodifen (suprahistaprodifen). All derivatives show high affinity for 3H-mepyramine labeled bovine aortic H1-receptor binding sites with the following order of potency: suprahistaprodifen dimethylhistaprodifen methylhistaprodifen...
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