Biochem/physiol Actions
Cholecystokinin is expressed in the gastrointestinal tract and the central nervous system. Cholecystokinin receptor type 2 (CCK2) is a GPCR that is highly expressed in brain and spinal cord. CCK2 is implicated in many brain processes, including mood, anxiety, and pain, through its modulation of GABA neurotransmission.
LY225910 is a potent, selective CCK2 antagonist. LY225910 blocks agonism of CCK2 by CCK-8S, the peptide agonist. LY225910 has been measured in multiple systems, including GABA efflux from cortical cultures, depolarization of spinal cord neurons (via potassium conductance), modulation of excitatory postsynaptic potentials (EPSPs) in nucleus accumbens slices, and enhancement of morphine analgesia.
LY 225910 is a potent, selective CCK2 antagonist.
Features and Benefits
This compound is featured on the Cholecystokinin and Gastrin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | off-white |
| solubility | DMSO: >20 mg/mL |
| originator | Eli Lilly |
| storage temp. | 2-8°C |
| SMILES string | CC(C)Oc1cccc(c1)N2C(CCc3c[nH]c4ccc(Br)cc34)=Nc5ccccc5C2=O |
| InChI | 1S/C27H24BrN3O2/c1-17(2)33-21-7-5-6-20(15-21)31-26(30-25-9-4-3-8-22(25)27(31)32)13-10-18-16-29-24-12-11-19(28)14-23(18)24/h3-9,11-12,14-17,29H,10,13H2,1-2H3 |
| InChI key | KUECXUACQOYKNB-UHFFFAOYSA-N |
