BPDBA

BPDBA is an inhibitor of betaine/GABA transporter 1 (BGT1; IC₅₀ = 20 µM) and an antagonist of sigma non-opioid intracellular receptor 1 (σ₁ receptor; K_i = 2.6 nM).^1,2 It is selective for BGT1 over GABA transporter 1 (GAT1), GAT2, GAT3, and excitatory amino acid transporter 3 (EAAT3; IC₅₀s = >100 µM for all) and for the σ₁ receptor over sigma intracellular receptor 2 (σ₂ receptor; K_i = 205 nM). BPDBA (10 µM) inhibits betaine-induced increases in the levels of the tight junction proteins claudin-1, claudin-4, and occludin in human skin ex vivo.³ BPDBA (30 µg/animal) decreases mechanical allodynia in a rat model of neuropathic pain, an effect that can be reversed by the σ₁ receptor agonist PRE-084.²

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1. Kragholm, B., Kvist, T., Madsen, K.K., et al. Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile. Biochem. Pharmacol. 86(4), 521-528 (2013).

2. Navarrete-Vázquez, G., Morales-Galindo, D.K., Ortiz-Andrade, R., et al. Antiallodynic effect of a novel sigma-1 receptor antagonist N-(1-benzylpiperidin-4-yl)-2,4-dichlorobenzamide (Dicloperidine): Synthesis and combined bioevaluation. Neurosci. Lett. 883, 138666 (2026).

3. El-Chami, C., Foster, A.R., Johnson, C., et al. Organic osmolytes increase expression of specific tight junction proteins in skin and alter barrier function in keratinocytes. Br. J. Dermatol. 184(3), 482-494 (2021).