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The tert-butyl moiety of compound 2 points to TM7 and makes hydrophobic contacts with A350 6.39b and K351 6.40b , replacement at the C-3 position by polar functional groups caused a dramatic decline in its potency and efficacy 38

FEBS Lett (1995) 374(1):4852.10.1016/0014-5793(95)01072-M 19 DrachmanJGKaushanskyK

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