Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10911 |
H3 receptor antagonist 1
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist. | |||
T14087 |
ABT-239
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
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。 | |||
T79500 |
KSK94
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
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。 | |||
T79499 |
KSK68
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
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。 | |||
T26643 |
Aplysamine-1
Aplysamine |
||
Aplysamine-1 is an antagonist of histamine H3 receptor. | |||
T60340 |
ROS 234
|
||
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]. | |||
T61603 | H3R antagonist 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]. | |||
T78734 |
Sigma-1 receptor antagonist 5
|
Sigma receptor | GPCR/G Protein |
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。 | |||
T10462L |
Bavisant dihydrochloride hydrate
JNJ31001074AAC |
Others | Others |
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 |