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Neuroscience - Histamine H1 Receptors

Neurons are the foundations of the sophisticated neural networks. Neurotransmitters such as dopamine, glutamate, and GABA, are crucial signaling molecules for the delivery of neuronal signals. Neurons synthesize/import neurotransmitters, and store them in presynaptic vesicles. A neuronal impulse is propagated by the vesicles released from presynaptic neurons.

Neurotransmitter receptors function via various G-protein coupled and G-protein independent mechanisms that activate downstream intracellular signaling pathways such as cAMP/PKA, PI3K/AKT, phospholipase A2, and phospholipase C pathways. For instance, dopamine receptors act through adenylate cyclase to activate PKA and other signaling molecules, thereby mediate gene expression through the actions of CREB and other transcription factors. Other neurotransmitters such as NMDAR or AMPAR are associated with ion channels that control flux of Ca2+ and Na+, thus propagating the action potential across the post-synaptic neuron.

Dysfunctions in GABAergic/glutamatergic/serotonergic/dopaminergic pathways result in a broad range of neurological disorders such as chronic pain, neurodegenerative diseases, and insomnia, as well as mental disorders including schizophrenia, bipolar disorder, depression, and addiction.

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  1. Clemizole hydrochloride
    Catalog No. :
    A3316
    H1 histamine receptor antagonist
    Clemizole Hcl is a H1 histamine receptor antagonist. Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.
  2. 2-Pyridylethylamine dihydrochloride
    Catalog No. :
    B7072
    Histamine H1 receptor agonist
    New Product
  3. Azelastine HCl
    Catalog No. :
    B1568
    Potent, second-generation, selective, histamine receptor antagonist
    Azelastine HCl is a potent, second-generation, selective, histamine antagonist.
  4. Rupatadine Fumarate
    Catalog No. :
    B1566
    Inhibitor of PAF and histamine (H1) receptor
    Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. Phase 2.
  5. Pemirolast potassium
    Catalog No. :
    B1563
    Histamine H1 receptor antagonist
    Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
  6. Hydroxyzine 2HCl
    Catalog No. :
    B1549
    Histamine H1-receptor antagonist
    Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.
  7. Cyclizine 2HCl
    Catalog No. :
    B1548
    Histamine H1 receptor antagonist
    Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
  8. Cetirizine DiHCl
    Catalog No. :
    B1547
    H1 receptor inverse agonist
    Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
  9. Paliperidone
    Catalog No. :
    A8496
    Dopamine receptor antagonist
    Paliperidone is a SR (5-HT2) receptor antagonist and D2DR inhibitor.
  10. Loratadine
    Catalog No. :
    A2960
    Peripheral HH1R antagonist
    Peripheral histamine H1 receptor antagonist (Ki = 35 nM); devoid of central effects.

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