G-protein coupled receptors (GPCRs) are a diverse super-family of proteins located within the plasma membrane of eukaryotic cells which have a common architecture consisting of seven-transmembrane (7-TM) segments, connected by extracellular (ECL) and intracellular (ICL) loops. They differ from other 7-TM proteins in their ability to activate guanine-nucleotide binding proteins or β-arrestin and so initiate a signaling cascade. Therefore, they are among the most important pharmaceutical drug targets,. GPCRs are activated by a wide variety of stimulants, including light, odorant molecules, peptide and non-peptide neurotransmitters, hormones, growth factors and lipids, and control a wide variety of physiological processes including sensory transduction, cell–cell communication, neuronal transmission, and hormonal signaling. Upon activation by a stimulant (binding or conformational change of ligand), the conformation of the receptor is altered, which can result into two principal signal transduction pathways involving the G protein-coupled receptors: the cAMP signal pathway and the phosphatidylinositol signal pathway.
Analysis of the human genome revealed at least 799 unique GPCRs. One widely adopted scheme classify the GPCRs into six families, with the most important and extensively studied being: family A (Rhodopsin-like); family B (Secretin); family C (Metabotropic glutamate/pheromone); family D (Fungal mating hormone); family E (Cyclic AMP); family F (Frizzled/Smoothened).
 Modeling the 3D structure of GPCRs: advances and application to drug discovery. Becker O.M., Shacham S., Marantz Y., Noiman S. Current Opinion in Drug Discovery & Development 2003, 6(3):353-361.
 G protein coupled receptors – exploiting flexible conformations. K.L. Chapman, J..BC.Findlay, G.K. Kinsella. Eur. Pharm. Rev. 2012, 6
 Tools for GPCR drug discovery. R. Zhang, X. Xie. Acta Pharmacologica Sinica (2012) 33: 372–384
 G proteins: transducers of receptor-generated signals. Gilman A.G. Annu. Rev. Biochem. 1987, 56, 615–49
 P. Joost, A. Methner. Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands. Gen. Biol. 2002, 3, 0063.
|Axon ID||Name||Description||From price|
|1575||5-HT6 antagonist 29||Selective brain penetrant 5-HT6 receptor antagonist||€90.00|
|2155||A 841720||Non-competitive mGluR1 antagonist||€85.00|
|1990||A 943931||Selective histamine H4 receptor antagonist||€75.00|
|1179||A1B1 hydrochloride||CCR1 antagonist||€125.00|
|1510||ABT 239 tartrate||H3 antagonist/inverse agonist||€135.00|
|1250||ABT 724 trihydrochloride||D4 agonist||€85.00|
|1579||ACR 16 hydrochloride||Dopaminergic stabilizer that stabilizes psychomotor activity||Inquire|
|1188||Adenosine amine congener||Adenosine A1 agonist||€125.00|
|1751||ADL 5859||Selective δ-opioid receptor agonist||€115.00|
|1492||Agomelatine||Melatonin agonist; 5-HT2C antagonist||€75.00|
|1335||AH 001||Melatonin agonist||€80.00|
|1336||AH 002||Melatonin agonist||Inquire|
|2062||Alprostadil||Prostaglandin EP (1-4) receptor antagonist||€105.00|
|2367||AM 095 (parent compound)||Novel potent and selective LPA1 antagonist||€125.00|
|1218||AM 251||CB1 antagonist||€95.00|