2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor
  5. H3 Receptor Isoform
  6. H3 Receptor Antagonist

H3 Receptor Antagonist

H3 Receptor Antagonists (28):

Cat. No. Product Name Effect Purity
  • HY-12199B
    Pitolisant hydrochloride
    		Antagonist 99.96%
    Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  • HY-14111
    GSK189254A
    		Antagonist 98.59%
    GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
  • HY-119087
    JNJ-28583867
    		Antagonist
    JNJ-28583867 is an orally active and selective histamine H3 receptor antagonist (Ki=10.6 nM) and serotonin transporter (SERT) inhibitor (Ki=3.7 nM). JNJ-28583867 can be used in the research of depression.
  • HY-122171
    A-317920
    		Antagonist
    A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade.
  • HY-116386
    GSK334429
    		Antagonist
    GSK334429 is a selective and orally active non-imidazole histamine H3 receptor antagonist with a pKi of 9.49 against human H3 receptor. GSK334429 can be utilized in neurological research.
  • HY-101232
    Tiotidine
    		Antagonist 99.28%
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
  • HY-12195
    ABT-239
    		Antagonist 99.23%
    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 
  • HY-123532
    JNJ10191584
    		Antagonist 99.95%
    JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
  • HY-107566
    Conessine
    		Antagonist 99.87%
    Conessine, a steroidal alkaloid, is a potent and selective histamine H3 receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H3 receptor, respectively. Anti-malarial activity.
  • HY-106000
    GSK239512
    		Antagonist 98.93%
    GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD).
  • HY-12190
    JNJ-5207852
    		Antagonist ≥98.0%
    JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
  • HY-109968
    Irdabisant
    		Antagonist 99.38%
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment.
  • HY-14880
    Bavisant
    		Antagonist
    Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research.
  • HY-12206A
    Thioperamide maleate
    		Antagonist 98.26%
    Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM.
  • HY-14880B
    Bavisant dihydrochloride hydrate
    		Antagonist 99.26%
    Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research.
  • HY-U00076
    MK-0249
    		Antagonist 99.53%
    MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with an IC50 of 1.7 nM for human H3.
  • HY-107558
    JNJ10191584 maleate
    		Antagonist
    JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
  • HY-107562
    JNJ 10181457 dihydrochloride
    		Antagonist
    JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H3 antagonist which increases NE and ACh concentrations in rat frontal cortex. JNJ-10181457 can be used for neurological research.
  • HY-19881
    ABT-288
    		Antagonist
    ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. ABT-288 has Ki values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research..
  • HY-12190A
    JNJ-5207852 dihydrochloride
    		Antagonist
    JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.