AI Article Synopsis
- The study focused on synthesizing lipidated oxytocin (LOT) analogues with long alkyl chains, which were created to improve their effectiveness.
- The LOTs synthesized (LOT-4a-c and LOT-5a-c) did not activate OT and vasopressin receptors, but LOT-4c demonstrated a strong and lasting impact on social behavior in mice models representing autistic traits.
- These findings suggest that LOT-4c could potentially be developed as a prodrug for enhancing social behaviors in specific scenarios.
Article Abstract
In the course of our studies of hydrophobic oxytocin (OT) analogues, we newly synthesized lipidated OT (LOT-4a-c and LOT-5a-c), in which a long alkyl chain (C14-C16) is conjugated via a carbonate or carbamate linkage at the Tyr-2 phenolic hydroxy group and a palmitoyl group at the terminal amino group of Cys-1. These LOTs did not activate OT and vasopressin receptors. Among the LOTs, however, LOT-4c, having a C16-chain via a carbonate linkage at the phenolic hydroxyl group of the Tyr-2, showed very long-lasting action for the recovery of impaired social behavior in CD38 knockout mice, a rodent model of autistic phenotypes, whereas the effect of OT itself rapidly diminished. These results indicate that LOT-4c may serve as a potential prodrug in mice.
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| http://dx.doi.org/10.1016/j.bmc.2019.06.018 | DOI Listing |
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