AC-178335

AC-178335 is a pure somatostatin (SRIF) antagonist with an affinity constant (Ki) of 172 +/- 12 nM. AC-178335 blocks SRIF inhibition of adenylate cyclase in vitro (IC50 = 5.1 +/- 1.4 microM) . It induces GH release when given alone (50 micrograms intravenously) to anesthetized rats with or without pretreatment with a long-acting SRIF agonist.

C([C@@H](NC([C@H](NC([C@H](NC([C@@H](CC1=CC=CC=C1)NC([C@@H](CC2=CN=CN2)NC(C)=O)=O)=O)[C@@H](CC)C)=O)CCCNC(=N)N)=O)C(N[C@H](CC3=CC=CC=C3)C(N)=O)=O)C=4C=5C(NC4)=CC=CC5