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BP-554 maleate is a selective agonist of 5-HT1A receptor [1].

The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.

BP-554 maleate is a selective 5-HT1A receptor agonist. BP-554 showed higher affinity for 5-HT1A receptor than for 5-HT1-non-A, 5-HT2, α2-adrenergic, dopamine D2 and benzodiazepine receptors. In rat hippocampal membranes, BP-554 inhibited the activity of adenylate cyclase stimulated by forskolin [1].

In mice, BP-554 inhibited the accumulation of 5-hydroxytryptophan after decarboxylase inhibition and reduced the concentration of 5-hydroxy-indoleacetic acid in the brain. Also, BP-554 increased the levels of serum corticosterone and induced hypothermia [1]. The 5-HT1(A) receptor, 5-HT, brain-derived neurotrophic factor (BDNF) receptor trkB and BDNF formed an auto/paracrine loop to regulate the serotonergic phenotype. In rats, BP-554 dose-dependently increased amounts of neurons expressing serotonergic markers [2]. In monkeys, injection of BP554 into the primary visual cortex decreased multiunit activity (MUA) without influenced blood oxygen-level-dependent (BOLD) and local field potential (LFP) activity [3].

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