STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF DERIVATIVES OF AMINOTETRALINS AND OPEN-CHAIN ANALOGS IN RELATION TO BETA-ADRENOCEPTOR AND ALPHA-ADRENOCEPTOR AGONIST ACTIVITIES

  • 1 January 1976
    • journal article
    • research article
    • Vol. 223  (2) , 215-222
Abstract
Some derivatives of aminotetralins and their open chain analogs were tested for their ability to alter blood pressure and heart rate in anesthetized cats with both vagi nerves sectioned and their ability to relax tracheal smooth muscle of guinea pigs. TL-257 and JOD-213, tertiary amines, produced weak .alpha.-adrenoceptor stimulating activity while JOD-176 [5,6-dihydroxy-2-isopropylaminotetralin] and JOD-211, secondary amines, showed .beta.-adrenoceptor stimulating activity. Another compound, M-8 [5,6-dihydroxy-2-methylaminotetralin], an aminotetralin that is a secondary amine, produced .alpha. and .beta. adrenoceptor stimulating activity. The .beta.-adrenoceptor stimulating activities of M-8 and JOD-176 showed more specificity for .beta.2-adrenoceptors than for .beta.1-adrenoceptors.

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