Biochem/physiol Actions

Reversible: yes

Primary TargetD2

General description

A tetrahydroisoquinoline-7-carbonitrile based compound that acts as a negative allosteric modulator of dopamine D2 receptor (estimated affinity (K_b) = 145-416 nM in GTP γS binding and in cell based functional assays). Its allosteric action requires D2R dimers. Shown to significantly reduce dopamine potency (8 to 16 fold), but acts as a partial antagonist and allows some dopamine action to remain. Displays features similar to orthosteric D2R antagonists and its highly stable tetrahydroisoquinoline (THIQ) moiety occupies the orthosteric site. Also exhibits bitopic mode of interaction with D2R. Binds to one promoter of D2R dimer in a bitopic mode and modulates the action of dopamine at the other. A G2A mutation in D2R causes a 9-fold reduction in its affinity and 5-fold decrease in negative cooperativity.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Dopamine D2 Receptor Antagonist, SB26965, is a negative allosteric modulator of dopamine D2 receptor (estimated affinity (K_b) = 145 - 416 nM in GTPgS binding and in cell based functional assays).

A tetrahydroisoquinoline-7-carbonitrile based compound that acts as a negative allosteric modulator of dopamine D2 receptor (estimated affinity (K_b) = 145-416 nM in GTP γS binding and in cell based functional assays). Its allosteric action requires D2R dimers. Shown to significantly reduce dopamine potency (8 to 16 fold), but acts as a partial antagonist and allows some dopamine action to remain. Displays features similar to orthosteric D2R antagonists and its highly stable tetrahydroisoquinoline (THIQ) moiety occupies the orthosteric site. Also exhibits bitopic mode of interaction with D2R. Binds to one promoter of D2R dimer in a bitopic mode and modulates the action of dopamine at the other. A G2A mutation in D2R causes a 9-fold reduction in its affinity and 5-fold decrease in negative cooperativity.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Lane, J., et al. 2014. Nat. Chem. Biol.10, 745.

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)