VU 10010 is a selective allosteric potentiator of M4 acetylcholine receptors. VU 10010 had no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5. VU 10010 is selective for M4 relative to other mAChRs - this compound does not displace [3H]NMS binding at any (rM1, rM2, rM3 and rM5) mAChR subtype. VU10010 was not found to be centrally active. It suffers from poor physiochemical properties. Novel analogs of VU10010 are CNS penetrant following systemic administration.

CDPPB is a drug used in scientific research which acts as a positive allosteric modulator (PAM) selective for the metabotropic glutamate receptor subtype mGluR5 CDPPB was shown to be the first systemically available mGlu5 PAM, thus allowing for behavioral assessment in antipsychotic models, including reversal of amphetamine-induced hyperlocomotion and reversal of deficits in prepulse inhibition, both of which have translational validity in patients with schizophrenia eliciting positive symptoms and cognitive deficits in sensorimotor gating, respectively. CDPPB was shown to be efficacious in both of these models at moderate subcutaneous (s.c.) doses between 10 and 30 mg/kg. Numerous in vivo studies using CDPPB have recently surfaced which continue to add evidence and support for the potential to treat CNS disorders associated with aberrant NMDA receptor function, including the cognitive impairments and negative symptoms of schizophrenia.

Targeting alpha7 neuronal acetylcholine receptors (nAChRs) with selective agonists and positive allosteric modulators (PAMs) is considered a therapeutic approach for managing cognitive deficits in schizophrenia and Alzheimer's disease. A-867744 is a novel type II positive allosteric modulator of α7 nAChR, which was developed by Abbott Laboratories, and has a good potency and selectivity.