TABLE 1

Amino acid sequences and affinity values (Ki) of the investigated ligands

Substitutions and/or modifications of the amino acid sequence of OT are indicated in boldface type; the superscript numbers indicate the position of the residue in the peptide sequence.

AnalogSequenceKi for:
mOTRmV1amV1b
nM ± %CV
OTCys1, Tyr2, Ile3, Gln4, Asn5, Cys6, Pro7, Leu8, Gly-NH290.83 ± 1720.38 ± 2636.32 ± 7
AVPCys1, Tyr2, Phe3, Gln4, Asn5, Cys6, Pro7, Arg8, Gly-NH290.87 ± 81.11 ± 270.43 ± 12
dLVTdCys1, Tyr2, Ile3, Gln4, Asn5, Cys6, Pro7, Lys8, Gly-NH290.43 ± 203.39 ± 280.82 ± 7
TGOTCys1, Tyr2, Ile3, Thr4, Asn5, Cys6, Gly7, Leu8, Gly-NH290.04 ± 32>1000>10,000
AtosibandCys1, DTyr(Et)2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn8, Gly-NH291.29 ± 46>1000>1000
 OTA1d(CH2)51, Tyr(Me)2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn8, Tyr-NH290.13 ± 4234.3 ± 33374.9 ± 20
 OTA2desGly-NH2,d(CH2)51, Tyr(Me)2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn80.27 ± 25232 ± 48>10,000
 OTA3desGly-NH2,d(CH2)51, DTyr2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn81.24 ± 36>10,000>10,000
LVAPhenylac1, DTyr(Me)2, Phe3, Gln4, Asn5, Arg6, Pro7, Arg83.90 ± 300.10 ± 199.66 ± 12
Manning compoundd(CH2)51, Tyr(Me)2, Phe3, Gln4, Asn5, Cys6, Pro7, Arg8, Gly-NH2942.6 ± 181.72 ± 2873.87 ± 9
SR4905913.2 ± 190.94 ± 2297.35 ± 12
  • d, deamino; d(CH2)5, β-mercapto-β,β-penthamethylenepropionic; desGly-NH2, desglycineamide; DTyr(Et), O-ethyl-d-tyrosine; Orn, ornithine; Phenylac, phenylacetyl; Tyr(Me), O-methyltyrosine.