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GPCR/G protein

GPCRs (G-protein coupled receptors) are a major subcategory of signaling pathways that play a crucial role in transmitting signals from outside the cell to within. These receptors are involved in a wide range of physiological processes including sensory perception, neurotransmission, hormonal regulation, and immune responses.

When a ligand binds to a GPCR, it causes a conformational change in the receptor that activates an associated G-protein. The activated G-protein then triggers a cascade of intracellular signaling events that ultimately lead to a specific cellular response.

GPCRs are a diverse family of proteins that can be classified into different subtypes based on their structure and function. Some examples of GPCR subtypes include rhodopsin-like, secretin-like, and metabotropic glutamate receptors.

Dysregulation of GPCR signaling pathways has been implicated in a variety of diseases, including cancer, cardiovascular disorders, and neurological conditions. Therefore, understanding the mechanisms underlying GPCR/G protein signaling is essential for the development of novel therapeutics targeted at these pathways.

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CGP 20712 dihydrochloride, B6552, C23H25F3N4O5·2HCl, β1 antagonist,highly potent and selective
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Nisoxetine hydrochloride, B6553, C17H21NO2·HCl, noradrenalin uptake inhibitor
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N-Desmethylclozapine, B6545, C17H17ClN4, 5-HT2C serotonin receptor antagonist
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RS 16566 dihydrochloride, B6548, C18H23ClN4O·2HCl, ligand for the (R)-zacopride binding site
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LY 225910, B6550, C27H24BrN3O2, CCK2 receptor antagonist
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AH 11110 hydrochloride, B6541, C21H26N2O2·HCl, α1B-AR ligand,subtype-selective
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Spiperone hydrochloride, B6540, C23H26FN3O2·HCl, 5-HT2A serotonin and selective D2-like dopamine receptor antagonist
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Pindolol, B6539, C14H20N2O2, β-adrenoceptor antagonist with partial agonist activity
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RS 56812 hydrochloride, B6535, C18H21N3O2·HCl, 5-HT3 partial agonist
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RS 67506 hydrochloride, B6536, C18H28ClN3O4S·HCl, potent and selective 5-HT4 partial agonist

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