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Table 1 Summary of inhibitiory constants for angiotensin IV and LVV-hemorphin 7 and their analogues for IRAP

From: Development of cognitive enhancers based on inhibition of insulin-regulated aminopeptidase

Angiotensin IV and analogues

 

Reference

Ki (nM) *

   Val-Tyr-Ile-His-Pro-Phe

[21]

113

   Nle-Tyr-Ile-His-Pro-Phe

[21]

340

   Val-Tyr-Ile-Cys-Pro-Cys

[49]

25.8†

   Val-Tyr-Ile-[AMPAA]

[49]

43.6†

   Valψ(CH2NH2)-Tyr-Valψ(CH2NH2)-His-Pro-Phe (divalinal-AT4)

[21]

2300

   β2hVal-Tyr-Ile-His-Pro-Phe

[51]

26‡

LVV-hemorphin 7 and analogues

   Leu-Val-Val-Tyr-Pro-Trp-Thr-Gln-Arg-Phe

[48]

196

   Leu-Val-Val-Tyr-Pro-Trp-Thr-Gln-Arg-Phe

[21]

845

   Val-Tyr-Pro-Trp-Thr-Gln-Arg-Phe

[48]

56

   Leu-Val-Val-Tyr-Pro-Trp-Thr

[48]

560

   Val-Tyr-Pro-Trp-Thr

[48]

112

   Val-Tyr-Pro

[48]

620

  1. *Data obtained using HEK293 cells transiently transfected with insulin-regulated aminopeptidase and L-Leu-pNA as substrate. †Comparative angiotensin IV Ki data not reported. ‡Angiotensin IV Ki reported as 56 nM in this assay.