A cyclic analogue selective for the NKB specific binding site on rat brain synaptosomes

The cyclic analogue of NKB, [Cys2,Cys5]NKB is as active as SP and NKB in the guinea-pig ileum bioassay. Furthermore, [Cys2,Cys5]NKB is a selective substrate for the [3H]NKB specific binding site on rat cortical synaptosomes. Its binding potencies for [3H]NKB and 125I-BHSP binding sites, IC50 = 5.2 nM and 3.4 microM respectively were close to those observed for NKB.