Lipo-oxytocin-1
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Chemical and physical data | |
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Formula | C75H126N12O14S2 |
Molar mass | 1484.02 g·mol−1 |
Lipo-oxytocin-1 (LOT-1) is a synthetic peptide and derivative of oxytocin that acts as an agonist of the oxytocin receptor.[1] The lipidation strategy was applied to oxytocin to create a new peptide with improved pharmacokinetics.[1] LOT-1 consists of oxytocin conjugated with two palmitoyl groups.[1] After adjusting for molecular weight (LOT-1 is ~1.5x the weight of oxytocin), oxytocin and LOT-1 are equipotent.[1] In addition, LOT-1 appears to have a significantly longer duration of effect relative to that of oxytocin.[1] It has yet to be determined whether LOT-1 possesses improved blood-brain-barrier permeability relative to oxytocin.[1]
See also
- Carbetocin
- Demoxytocin
- Merotocin
- Palmitoylation
References
- ^ a b c d e f Mizuno A, Cherepanov SM, Kikuchi Y, Fakhrul AA, Akther S, Deguchi K, Yoshihara T, Ishihara K, Shuto S, Higashida H (2015). "Lipo-oxytocin-1, a Novel Oxytocin Analog Conjugated with Two Palmitoyl Groups, Has Long-Lasting Effects on Anxiety-Related Behavior and Social Avoidance in CD157 Knockout Mice". Brain Sci. 5 (1): 3–13. doi:10.3390/brainsci5010003. PMC 4390788. PMID 25612002.
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- Agonists: Peptide: Aspartocin
- Carbetocin
- Cargutocin
- Demoxytocin
- Lipo-oxytocin-1
- Merotocin
- Nacartocin
- Oxytocin
- PF-06478939
- PF-06655075 (PF1)
- TGOT
- Vasotocin (argiprestocin); Non-peptide: CA7
- LIT-001
- TC OT 39
- WAY-267464
- WJ0679
- Antagonists: Peptide: Atosiban
- Tocinoic acid; Non-peptide: Barusiban
- Cligosiban
- Epelsiban
- Erlosiban
- IX-01
- L-368,899
- L-371,257
- L-372,662
- Nolasiban
- Retosiban
- SSR-126768
- WAY-162720
- Catabolism inhibitors: Amastatin
- Bestatin (ubenimex)
- EDTA
- L-Methionine
- Leupeptin
- o-Phenanthroline
- Phosphoramidon
- Puromycin
V1A |
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V1B |
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V2 |
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Unsorted |
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- Carrier proteins: Neurophysin (I, II)
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