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Neuroscience - Voltage-gated Potassium (KV) Channels - 5-HT2 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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 Paper Citing APExBIO Products  Ongoing Clinical Trials  Solubility in DMSO  Solubility in Water  Solubility in Ethanol  Solubility in Dimethyl Formamide
  1. Ketanserin
    B2248 Ketanserin
    Target: 5-HT2 Receptors
    Summary: specific 5-HT2A serotonin receptor antagonist
      ≥39.5 mg/mL
  2. Amitriptyline HCl
    B2231 Amitriptyline HCl
    Target: Trk Receptors|5-HT2 Receptors|Norepinephrine transporter|5-HT Transporters
    Summary: Serotonin /norepinephrine receptor/5-HT4/5-HT2 inhibitor
      ≥15.693 mg/mL
  3. Pizotifen Malate
    B2007 Pizotifen Malate
    Target: 5-HT2 Receptors|D2 Receptors
    Summary: 5-HT receptor antagonist
      ≥21.48 mg/mL
  4. Pizotifen
    B1206 Pizotifen
    Target: 5-HT2 Receptors
    Summary: Highly selective 5-HT receptor blocking agent
      ≥14.77 mg/mL
  5. Lurasidone HCl
    B1477 Lurasidone HCl
    Target: 5-HT2 Receptors|D2 Receptors|5-HT1 Receptors|5-HT7 Receptors
    Summary: Dopamine D2/5-HT2A/5-HT7/5-HT1A inhibitor
      ≥11.11 mg/mL
  6. Quetiapine Fumarate
    B1490 Quetiapine Fumarate
     1 Citation
    Target: 5-HT2 Receptors|D1 and D5 Receptors|D2 Receptors|D3 Receptors|5-HT1 Receptors|5-HT7 Receptors
    Summary: Dopamine receptor antagonist
      ≥11.03 mg/mL
  7. Loxapine
    B1001 Loxapine
     1 Citation
    Target: 5-HT2 Receptors
    Summary: 5-HT receptor antagonist
      soluble in dmso
  8. Olanzapine
    B2240 Olanzapine
    Target: 5-HT2 Receptors|D2 Receptors
    Summary: Antagonist of 5-HT2A and dopamine D2 receptors
      ≥15.6 mg/mL
  9. Clozapine
    B2235 Clozapine
    Target: 5-HT2 Receptors|D1 and D5 Receptors|D2 Receptors|D3 Receptors|5-HT1 Receptors|D4 Receptors
    Summary: 5-HT receptor antagonist
      ≥14.95 mg/mL
  10. Cisapride
    B1198 Cisapride
    Target: Voltage-gated Potassium (KV) Channels|5-HT4 Receptor
    Summary: 5-HT4 receptor agonist
      ≥23.3 mg/mL

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