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.
- Clemizole hydrochlorideCatalog No. :A3316H1 histamine receptor antagonistClemizole 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-Pyridylethylamine dihydrochlorideCatalog No. :B7072Histamine H1 receptor agonistNew Product
- Azelastine HClCatalog No. :B1568Potent, second-generation, selective, histamine receptor antagonistAzelastine HCl is a potent, second-generation, selective, histamine antagonist.
- Rupatadine FumarateCatalog No. :B1566Inhibitor of PAF and histamine (H1) receptorRupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. Phase 2.
- Pemirolast potassiumCatalog No. :B1563Histamine H1 receptor antagonistPemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
- Hydroxyzine 2HClCatalog No. :B1549Histamine H1-receptor antagonistHydroxyzine 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.
- Cyclizine 2HClCatalog No. :B1548Histamine H1 receptor antagonistCyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
- Cetirizine DiHClCatalog No. :B1547H1 receptor inverse agonistCetirizine 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.
- PaliperidoneCatalog No. :A8496Dopamine receptor antagonistPaliperidone is a SR (5-HT2) receptor antagonist and D2DR inhibitor.
- LoratadineCatalog No. :A2960Peripheral HH1R antagonistPeripheral histamine H1 receptor antagonist (Ki = 35 nM); devoid of central effects.