Receptor Binding Profiles of Antidepressants

Legend:

• pKi ~X.X: Affinity with a pKi value of approximately X.X.
• SERT: Serotonin transporter.
• NET: Norepinephrine transporter.
• DAT: Dopamine transporter.
• 5-HTx: Various subtypes of serotonin receptors.
• α1, α2: Adrenergic receptors.
• H1: Histamine H₁ receptor.
• M1: Muscarinic acetylcholine receptor.
• Notes: Important information about the medication's mechanism of action or special properties.

Explanations of the Medications:​

1. Selective Serotonin Reuptake Inhibitors (SSRIs)​

• Medications: Fluoxetine, Sertraline, Paroxetine, Citalopram, Escitalopram
• Mechanism of Action: Selectively inhibit SERT, increasing serotonin levels in the synaptic cleft.
• Indications: Treatment of depression, anxiety disorders, obsessive-compulsive disorder (OCD).
• Side Effects: Nausea, sleep disturbances, sexual dysfunction.

2. Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)​

• Medications: Venlafaxine, Duloxetine
• Mechanism of Action: Inhibit SERT and NET, increasing serotonin and norepinephrine levels.
• Indications: Depression, generalized anxiety disorder, neuropathic pain.
• Side Effects: Nausea, sweating, increased blood pressure.

3. Tricyclic Antidepressants (TCAs)​

• Medications: Amitriptyline, Nortriptyline, Imipramine, Desipramine, Clomipramine
• Mechanism of Action: Inhibit SERT and/or NET and act on various receptors (H1, M1, α1).
• Indications: Severe depression, chronic pain, migraine prophylaxis.
• Side Effects: Sedation, anticholinergic effects, orthostatic hypotension.

4. Norepinephrine-Dopamine Reuptake Inhibitor (NDRI)​

• Medication: Bupropion
• Mechanism of Action: Inhibits NET and DAT, increasing norepinephrine and dopamine levels.
• Indications: Depression, smoking cessation.
• Side Effects: Insomnia, dry mouth, increased seizure risk.

5. Noradrenergic and Specific Serotonergic Antidepressant (NaSSA)​

• Medication: Mirtazapine
• Mechanism of Action: Antagonist at presynaptic α2-adrenergic receptors and 5-HT₂/5-HT₃ receptors; increases the release of norepinephrine and serotonin.
• Indications: Depression with sleep disturbances and loss of appetite.
• Side Effects: Strong sedation, weight gain.

6. Selective Norepinephrine Reuptake Inhibitor (NRI)​

• Medication: Reboxetine
• Mechanism of Action: Selectively inhibits NET, increasing norepinephrine levels.
• Indications: Depression; off-label use for ADHD.
• Side Effects: Sleep disturbances, dry mouth, increased blood pressure.

7. Agomelatine​

• Mechanism of Action: Agonist at melatonin receptors (MT1, MT2); antagonist at 5-HT₂C receptors.
• Indications: Depression with sleep disturbances, circadian rhythm disorders.
• Side Effects: Elevated transaminases (liver enzymes), headaches, dizziness.

Important Notes:​

• Data Variability: Exact pKi values can vary depending on the study.
• Clinical Relevance: The effectiveness of an antidepressant depends not only on affinity to transporters and receptors but also on individual factors.
• Side Effects: Antidepressants can have different side effects depending on their receptor profile.

Disclaimer: This table is for informational purposes only and does not replace professional advice from a healthcare provider. For questions about therapy or medications, please consult your doctor or pharmacist.

Sources:​

• PDSP Ki Database (University of North Carolina)
• Stahl's Essential Psychopharmacology
• Current scientific literature and pharmacological databases
  

PDF print version see attachment: