RESUMO
A four-step synthesis of 2-chlorodopamine (2b) is presented as well as methods for the syntheses of the N-methyl, ethyl, and n-propyl analogues (2c-e). Compounds 2b and 2c were essentially equipotent to dopamine for increasing renal blood flow in anesthetized dogs that had been treated with the alpha-adrenergic antagonist phenoxybenzamine. The increases in renal blood flow were blocked by the DA1 antagonist (R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine. Compounds 2d and 2e were significantly less potent than dopamine in the same model; the increases in renal blood flow were attenuated by propranolol and blocked by a combination of propranolol and (R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine. The significance of an o-chloro substituent on dopamine analogues for the activation of the DA1 receptor is briefly discussed.
Assuntos
Dopamina/análogos & derivados , Circulação Renal/efeitos dos fármacos , Vasodilatação/efeitos dos fármacos , Animais , Benzazepinas/farmacologia , Fenômenos Químicos , Química , Cães , Dopamina/síntese química , Dopamina/farmacologia , Feminino , Rim/irrigação sanguínea , Masculino , Propranolol/farmacologia , Relação Estrutura-AtividadeRESUMO
Pulmonary function data were compared with smoking history and past personal and family history of asthma, hay fever and eczema in apparently healthy males age 30 to 39. Mean values for FEV1 and MMEF were significantly lower in smokers with a positive allergic history compared to non-allergic smokers.
