Neuroscience
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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A3317 Clozapine N-oxide (CNO)1 CitationTarget: DREADD LigandsSummary: Metabolite of clozapine, used in chemogenetics.
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A3423 Galanthamine2 CitationTarget: AChESummary: Acetylcholinesterase inhibitor
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A3612 MK-0974Target: CGRP receptorsSummary: CGRP receptor antagonist
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A3680 OlcegepantTarget: CGRP receptorsSummary: Non-peptide receptor of CGRP,first potent and selective
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A3727 Pitolisant hydrochlorideSummary: Nonimidazole inverse agonist
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A3811 SEA04004 CitationTarget: Na /Ca2 Exchangers (NCXs)Summary: Specific inhibitor of Na+/Ca2+ exchange
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A1134 Agouti-related Protein (AGRP) (25-82), humanTarget: Melanocortin (MC) ReceptorsSummary: Agouti-related peptide(25-82)
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A3136 A-740003Target: P2X ReceptorsSummary: P2X7 receptor antagonist
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B2235 ClozapineTarget: 5-HT2 Receptors|D1 and D5 Receptors|D2 Receptors|D3 Receptors|5-HT1 Receptors|D4 ReceptorsSummary: 5-HT receptor antagonist
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B2240 OlanzapineTarget: 5-HT2 Receptors|D2 ReceptorsSummary: Antagonist of 5-HT2A and dopamine D2 receptors