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.
| Analog | Sequence |
Ki for: |
||
|---|---|---|---|---|
| mOTR | mV1a | mV1b | ||
| nM ± %CV | ||||
| OT | Cys1, Tyr2, Ile3, Gln4, Asn5, Cys6, Pro7, Leu8, Gly-NH29 | 0.83 ± 17 | 20.38 ± 26 | 36.32 ± 7 |
| AVP | Cys1, Tyr2, Phe3, Gln4, Asn5, Cys6, Pro7, Arg8, Gly-NH29 | 0.87 ± 8 | 1.11 ± 27 | 0.43 ± 12 |
| dLVT | dCys1, Tyr2, Ile3, Gln4, Asn5, Cys6, Pro7, Lys8, Gly-NH29 | 0.43 ± 20 | 3.39 ± 28 | 0.82 ± 7 |
| TGOT | Cys1, Tyr2, Ile3, Thr4, Asn5, Cys6, Gly7, Leu8, Gly-NH29 | 0.04 ± 32 | >1000 | >10,000 |
| Atosiban | dCys1, DTyr(Et)2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn8, Gly-NH29 | 1.29 ± 46 | >1000 | >1000 |
| OTA1 | d(CH2)51, Tyr(Me)2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn8, Tyr-NH29 | 0.13 ± 42 | 34.3 ± 33 | 374.9 ± 20 |
| OTA2 | desGly-NH2,d(CH2)51, Tyr(Me)2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn8 | 0.27 ± 25 | 232 ± 48 | >10,000 |
| OTA3 | desGly-NH2,d(CH2)51, DTyr2, Ile3, Thr4, Asn5, Cys6, Pro7, Orn8 | 1.24 ± 36 | >10,000 | >10,000 |
| LVA | Phenylac1, DTyr(Me)2, Phe3, Gln4, Asn5, Arg6, Pro7, Arg8 | 3.90 ± 30 | 0.10 ± 19 | 9.66 ± 12 |
| Manning compound | d(CH2)51, Tyr(Me)2, Phe3, Gln4, Asn5, Cys6, Pro7, Arg8, Gly-NH29 | 42.6 ± 18 | 1.72 ± 28 | 73.87 ± 9 |
| SR49059 | 13.2 ± 19 | 0.94 ± 22 | 97.35 ± 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.