h3 receptor (human)

PF-03654764 is an orally active, potent, and selective histamine H3 receptor antagonist with Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3. It is often co-administered with Fexofenadine for the treatment of allergic rhinitis.

MK-0249 is an orally active, selective and potent histamine H3 receptor antagonist (IC50: 1.7 nM) for the study of attention-deficit and hyperactivity disorders.

Bavisant (JNJ-31001074) is a selective and orally active Human H3 receptor antagonist. Bavisant can be used in research on mechanisms of action, involving wakefulness and cognition and the treatment for ADHD.

ABT-288 is a selective and potent H3 antagonist for the treatment of mild to moderate Alzheimer's dementia.

MK-0249 FA is an orally active, selective and potent histamine H3 inverse agonist for the study of attention deficit, hyperactivity disorder neurodivergent and cognitive disorders in adults.

OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea

JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor.

Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment.

JNJ-5207852 dihydrochloride is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor.

LML134 (LML-134) is an inverse agonist of Histamine 3 receptor (H3R)(hH3R cAMP and hH3R bdg with Kis of 0.3 nM and 12 nM).

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.

JNJ-10191584, a potent and selective antagonist at the histamine H4 receptor, has antiinflammatory and analgesic effects in animal studies of acute inflammation.

S 38093 is a brain-penetrant antagonist of the H3 receptor (Ki: 8.8 1.44 1.2 μM, for rat mouse human).

Pitolisant is a potent and selective nonimidazole inverse agonist that targets the recombinant human histamine H3 receptor, with a Ki of 0.16 nM.

Pitolisant oxalate is a potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor, exhibiting a Ki of 0.16 nM.

GSK189254A (GSK189254) is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2 M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0 G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......

A-940894 is a histamine H4 receptor antagonist with anti-inflammatory properties. A-940894 potently binds to both human and rat histamine H4 receptors and exhibits considerably lower affinity for the human histamine H1, H2, or H3 receptors. A-940894 has g

Bavisant (JNJ-310010740) dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition.

AChE-IN-14 is a potent cholinesterase inhibitor, acting on electric eel acetylcholinesterase (eeAChE) (IC50: 0.46 μM), human recombinant acetylcholinesterase (hAChE) (IC50: 0.48 μM) and equine serum butyrylcholinesterase (eqBuChE) (IC50: 0.44 μM). AChE-IN-14 has a high affinity for the human H3 receptor (H3R) (Ki: 159.8 nM) and can be used to study Alzheimer's disease.

JNJ 10191584 maleate (VUF6002 maleate) is an orally active and selective antagonist of H4 receptor (Ki = 26 nM). JNJ 10191584 maleate inhibits chemotaxis of eosinophils and mast cells (IC50 = 530 nM and 138 nM).

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].

Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

AZD5213 is a selective, competitive antagonist of the human H3 receptor, exhibiting a pK i of 9.3 against hH3R. It is utilized in the research of sleep and cognitive regulation.