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.
- B7043 Ro 90-7501Summary: Inhibitor of amyloid β42 (Aβ42) fibril assembly
- B7049 GT 2016Summary: H3 receptor antagonist
- B7053 TMPH hydrochlorideSummary: neuronal nicotinic ACh receptors (nAChRs) antagonist
- B7055 JNJ 10191584 maleateSummary: histamine H4 receptor silent antagonist
- B7058 Desmethyl-YM 298198Summary: mGlu1-selective antagonist
- B7059 YM 298198 hydrochlorideSummary: mGlu1 receptor antagonist
- B7061 LY 379268Summary: group II mGlu receptor agonist, highly selective
- B7071 Proxyfan oxalateSummary: histamine H3 receptor ligand
- B7076 VUF 5681 dihydrobromideSummary: histamine H3 receptor silent antagonist
- B7077 VUF 8430 dihydrobromideSummary: histamine H4 receptor full agonist