5-HT6 选择性抑制剂 | 拮抗剂

SB742457

SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

SB 271046 hydrochloride

SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pK_i of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.

Indophagolin

Indophagolin, a potent indoline-containing autophagy inhibitor with IC50 of 140 nM, antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively, also has a strong antagonistic effect on serotonin receptor 5-HT6 with IC50 of 1.0 μM.

Asenapine maleate

Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.

Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.

BRL-15572 Dihydrochloride

BRL-15572 is a 5-HT1D receptor antagonist with pK_i of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.