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.
- B7166 PNU 96415ESummary: dopamine D4 and serotonergic 5-HT2A receptor antagonist
- B7168 TC 2559 difumarateSummary: partial agonist of α4β2 nicotinic acetylcholine receptor
- B7205 Mecamylamine hydrochlorideSummary: nicotinic acetylcholine receptor antagonist
- B7213 CP 96345Summary: NK1 receptor antagonist
- B7217 Ro 64-5229Summary: mGlu2 antagonist
- B7243 NS 1738Summary: positive allosteric modulator of α7 nicotinic acetylcholine receptor
- B7258 A 841720Summary: mGluR1 antagonist, non-competitive
- B7282 PHA 568487Summary: α7 nicotinic acetylcholine receptor agonist
- B7285 VU 10010Summary: allosteric potentiator of M4 acetylcholine receptors
- B7324 CDPPBSummary: positive allosteric modulator of the mGlu5 receptor