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DAPTA is a peptide antagonist of chemokine (C-C motif) receptor 5 (CCR5).1 It inhibits CD4-dependent binding of HIV-1Ba-L and HIV-1CM235 gp120 envelope proteins to CCR5 (IC50s = 0.06 and 0.32 nM, respectively). DAPTA (0.1 mg/kg, i.p.) reduces marble burying and repetitive behavior, as well as decreases brain levels of IL-6, IL-9, and IL-17A, in the BTBR T+ Itpr3tf/J mouse model of autism spectrum disorder (ASD).2 It also reduces LPS-induced microglial activation and astrocyte hypertrophy in the dentate gyrus in a rat model of chronic neuroinflammation.3

1.Polianova, M.T., Ruscetti, F.W., Pert, C.B., et al.Chemokine receptor-5 (CCR5) is a receptor for the HIV entry inhibitor peptide T (DAPTA)Antiviral Res.67(2)83-92(2005) 2.Ahmad, S.F., Ansari, M.A., Nadeem, A., et al.DAPTA, a C-C chemokine receptor 5 (CCR5) antagonist attenuates immune aberrations by downregulating Th9/Th17 immune responses in BTBR T + Itpr3tf/J miceEur. J. Pharmacol.846100-108(2019) 3.Rosi, S., Pert, C.B., Ruff, M.R., et al.Chemokine receptor 5 antagonist D-Ala-peptide T-amide reduces microglia and astrocyte activation within the hippocampus in a neuroinflammatory rat model of Alzheimer's diseaseNeuroscience134(2)671-676(2005)

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