5-HT₆ Receptor Antagonist

Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic.

Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

SB 271046 Hydrochloride (SB 271046A) is a potent, selective, orally active and BBB-permeable 5-HT6 receptor antagonist with pK_i of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC₅₀=0.16 μM).

Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.

SB-399885 hydrochloride is a 5-HT₆ receptor antagonist.

Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic.

5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pK_i 7.24, human FAAH pIC₅₀ 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease.

Idalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a K_i value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.

SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pK_i values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties.

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC₅₀=140 nM). Indophagolin antagonizes the purinergic receptor P2X₄ as well as P2X₁ and P2X₃ with IC₅₀s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the G_q-protein-coupled P2Y₄, P2Y₆, and P2Y₁₁ receptors (IC₅₀s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT₆ (IC₅₀=1.0 μM) and a moderate effect on receptors 5-HT_1B, 5-HT_2B, 5-HT_4e, and 5-HT₇.

AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.

Olanzapine-d₃ (LY170053-d₃) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.

Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine mesylate has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine mesylate can be used in the research of Alzheimer's disease.

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (K_i=91 pM).

SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.

NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine₆ (5-HT₆) receptor antagonist, with an IC₅₀ of 7.2 nM and a K_i of 0.2 nM.

PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a K_i= 4-8 nM and an IC₅₀ of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.

Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.

Landipirdine (RO5025181; SYN120) is an orally active 5-HT6 and 5-HT2A receptors antagonist. Landipirdine can be used for the study of Parkinson disease.

5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.