h3 receptor antagonist 1

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂，也是一种TRPV1拮抗剂。

KSK68 是一种高效的 sigma-1 和 组胺 H3 受体双重拮抗剂，具有潜在的镇痛活性，对 H3 受体、sigma-1、sigma-2 受体有很高的亲和力。KSK68 可用于研究与疼痛相关的疾病。

KSK94 是一种特异性 H3 受体拮抗剂，抑制 H3、sigma-1、sigma-2受体 ，Ki值分别是7.9、2958 和 75.2 nM，可用于研究伤害性疼痛和神经性疼痛。

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change

H3R antagonist 6 (Compounds 3) (H3-2406) 是一种有效的组胺受体 3 (H3R) 拮抗剂，其IC50为 5.6 nM。经 18F 标记后，它表现出较高的放化产率、摩尔活性，并具有中等的脑摄取率，同时也存在与 Sigma-1 受体 (Sigma-1 receptor) 的非特异性结合。H3R antagonist 6 可用作正电子发射断层扫描 (PET) 成像的放射性配体，用于研究中枢神经系统 (CNS) 疾病。

Aplysamine-1 is an antagonist of histamine H3 receptor.

ROS 234 is a highly effective H3 antagonist, demonstrating a strong binding affinity (pK B) of 9.46 for the Guinea-pig ileum H3 receptor and a pKi of 8.90 for the Rat cerebral cortex H3 receptor. Additionally, it exhibits an ex vivo ED50 of 19.12 mg/kg (ip) in the Rat cerebral cortex. It should be noted that ROS 234 demonstrates limited central access, as reported in [1] and [2].

H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist. It exhibits inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, H3R antagonist 2 demonstrates favorable anti-neuropathic pain and memory-enhancing effects. Additionally, it can cross the blood-brain barrier (BBB) [1].

Sigma-1 receptor antagonist 5 (compound 12) 是一种 4-吡啶衍生物，既有镇痛活性也是 sigma 受体 (Ki=4.5 nM (σ1R)，10 nM (σ2R)) 及组胺 H3 (hH3R，Ki=7.7 nM，IC50=215 nM) 的拮抗剂。它能够抑制辣椒素引起的痛觉，并展现出对伤害性和神经性疼痛模型的显著疗效。