h3 receptor antagonist 1

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

ABT-239 is a novel, highly efficacious non-imidazole class histamine H3 receptor (H3R) antagonist and also acts as a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

KSK68 is a potent dual sigma-1 and histamine H3 receptor antagonist with potential analgesic activity and high affinity for H3 receptors, sigma-1, sigma-2 receptors.KSK68 can be used in the study of pain related diseases.

KSK94 is a specific H3 receptor antagonist that inhibits H3, sigma-1, and sigma-2 receptors , with Ki values of 7.9, 2958, and 75.2 nM, respectively, and can be used to study injurious pain and neuropathic pain.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action related to wakefulness and cognition, and it has potential as a treatment for ADHD. In a clinical trial, the mean change from baseline in the total ADHD-RS-IV score at day 42 was -8.8 in the placebo group versus -9.3, -11.2, and -12.2 in the bavisant 1 mg/day, 3 mg/day, and 10 mg/day groups, respectively; however, the change in the 10 mg/day group was not statistically superior to placebo (p=0.161). Statistical comparisons of the 1 mg/day and 3 mg/day groups with placebo based on a step-down closed testing procedure were not performed. Bavisant has completed a phase II ADHD trial, but no results have been reported [1]. Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2. IC50 Value: Target: H3 receptor in vitro.

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 with 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, it demonstrates favorable anti-neuropathic pain and memory-enhancing effects and can cross the blood-brain barrier (BBB) [1].

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].