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

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。