Serotonin 5-HT1a,b,d,e,f receptors

 Agonists:

Potent 5HT1a partial agonist properties: Aripiprazole, also the antipsychotics Brexpiprazole and Cariprazine

Antagonists: n/a

Distribution:

Central Nervous System

5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus

Can be presynaptic on the dendrites and cell bodies of serotonin neurons in the midbrain raphe

Postsynaptic 5HT1a receptors on pyramidal neurons in the cortex

Block Effect:

Decrease blood pressure and heart rate via a central mechanism, by inducing peripheral vasodilation, and by stimulating the vagus nerve

Decreased aggression, increased sociability, decreased impulsivity, inhibition of drug-seeking behavior, facilitation of sex drive and arousal, inhibition of penile erection, diminished food intake, prolongation of REM sleep latency, reversal of opioid-induced respiratory depression

Stimulate Effect:

5HT1a receptor stimulation in the cortex hypothetically stimulates downstream dopamine release in the striatum (by reducing glutamate release in the brainstem, which in turn fails to trigger the release of inhibitory GABA at dopamine neurons there).

Stimulation of presynaptic 5HT1a receptors (in the midbrain raphe) – allows the nigrostriatal dopamine neurons to be active and thus to release dopamine in the striatum – this theoretically mitigates EPS

 

SohoMD Office