Pridopidine selectively occupies sigma-1 rather than dopamine D2 receptors at behaviorally active doses.

ABSTRACT:

Rationale

Dopamine stabilizers have stimulatory actions under low dopamine tone and inhibitory actions under high dopamine tone without eliciting catalepsy. These compounds are dopamine D2 receptor (D2R) antagonists or weak partial agonists and may have pro-mnemonic and neuroprotective effects. The mechanism underlying their stimulatory and neuroprotective actions is unknown but could involve sigma-1R binding.

Objectives

The present study examined sigma-1R and D2R occupancy by the dopamine stabilizer pridopidine (ACR16) at behaviorally relevant doses in living rats.

Methods

Rats were administered 3 or 15 mg/kg pridopidine, or saline, before injection of the radiotracer (11)C-SA4503 (sigma-1R) or (11)C-raclopride (D2R). Some animals received 60 mg/kg pridopidine and we

SUBMITTER: Sahlholm K 

PROVIDER: S-EPMC4537502 | biostudies-literature | 2015 Sep

REPOSITORIES: biostudies-literature