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Neurobiology, Brain Anatomy, Neurotransmitter Synthesis, and Function
Section 2 of 3
Neurotransmitters are related to how the brain functions and how one feels. The most common neurotransmitters related to mental health are serotonin, norepinephrine, dopamine, acetylcholine, glutamate, and GABA (γ-aminobutyric acid).
Different medications are either agonists, partial agonists, antagonists, or inverse agonists. The neurotransmitter is the agonist. The antagonists are the opposite and are considered neutral. They are the cause of many side effects associated with psychiatric medications. The agonist imitates the action of the intended chemical for that receptor, thus creating a comparable response. The antagonist does the very opposite and elicits no response.
A partial agonist is somewhere in the middle; it is more than an antagonist but less than a full agonist. An inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either. The clinical significance of this action when compared to an antagonist is questionable.
The cytochrome P450 enzyme system is responsible for metabolism of psychiatric medications. Click below to learn more.
CYP1A2+CYP2D6
+CYP3A4
+Ligand-Gated Ion Channels
Psychiatric medications can target ligand-gated ion channels. Review the chart below:
NeurotransmitterLigand-gated ion channel receptor subtype directly targetedPharmacologic actionDrug classTherapeutic action
Acetylcholineα4β2 nicotinic receptors
Partial agonistNicotinic receptor partial agonist (NRPA) (varenicline)Smoking cessation
GABAGABAA benzodiazepine receptorsFull agonistBenzodiazepinesAnxiolytic
GABAGABAA non-benzodiazepine PAM sitesFull agonist”Z drugs”/hypnotics (zolpidem, zaleplon, zopiclone, eszopiclone)Improve insomnia
GlutamateNMDA NAM channel sites/Mg++ sitesAntagonistNMDA glutamate antagonist (memantine)Slowing progression in Alzheimer’s disease
Glutamate
NMDA open channel sitesAntagonistPCP (phencyclidine), ketamineHallucinogen anesthetic
Serotonin5HT3AntagonistAntidepressant (mirtazapine)
Unknown; reduce nausea
Serotonin5HT3
AntagonistAntiemetic Reduce chemotherapy-induced emesis
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