Summary of HTR2A
Activation of 5HT2A receptors is on the whole bad. The more receptors we have, the more likely they'll activate, so it's better to have fewer receptors. 5HT2A receptors are commonly found in platelets, the heart, joints, immune cells (monocytes), the vagus nerve (R) and brain (hypothalamus, brain stem, prefrontal) (R).
Activation of 5HT2A receptors can contribute to many problems, including anxiety, depression, fatigue, OCD, sleep problems, etc. However, some good effects include lowered heart rate and blood pressure and reduced inflammatory effects.
The Function of HTR2A
(Microbial infection) Acts as a receptor for human JC polyomavirus/JCPyV.
Recommended name:5-hydroxytryptamine receptor 2A
Serotonin receptor 2A
- RS12583882 (HTR2A) ??
- RS12584920 (HTR2A) ??
- RS17289394 (HTR2A) ??
- RS1923884 (HTR2A) ??
- RS2296972 (HTR2A) ??
- RS5443 (HTR2A) ??
- RS6311 (HTR2A) ??
- RS6313 (HTR2A) ??
- RS6314 (HTR2A) ??
- RS7322347 (HTR2A) ??
- RS7984966 (HTR2A) ??
- RS7997012 (HTR2A) ??
- RS9316233 (HTR2A) ??
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Top Gene-Substance Interactions
HTR2A Interacts with These Diseases
- Inositol - reduces 5HT2A receptor function (R),
- Zinc (R),
- Lectin avoidance?
- Feverfew (R)
- Ginkgo (R)
Inositol and fluoxetine reduce 5HT2A receptor function at the receptor-G protein level. In addition mI, and at high concentrations fluoxetine and imipramine, also reduces muscarinic acetylcholine receptors (R).
5HT2A receptors are in high concentration in the default mode network [DMN], which is overactive in depression (R).
This brain network is implicated in self-related thinking and mind wandering. Meditation leads to a reduced activity in the default mode network (R), which can help some of the negative effects of the 5HT2A receptors on depression.
The negative effects of the 5HT2A receptors seem to work through activating GSK3 (R) and stimulating calcium release inside cells. Therefore, GSK3 inhibitors such as lithium might help.
For the calcium release, magnesium may help. 5-HT2A has sialic acid in it, which is bound to by lectins. I wouldn't be surprised if this receptor was implicated in lectin sensitivity to a degree, given all of its associated symptoms. Lectins probably modify the receptor in some negative way in people who are susceptible.
- Microdosing LSD?
- Sialic Acid?
- MDMA (R) -in recent MDMA users, post-synaptic 5-HT(2A) receptor densities were significantly lower in all cortical areas studied,
However, other studies report a 50-percent increase in 5-HT2A receptors after six months of use (R).
Therefore, it may be best to stay away from it. Agmatine supplements may activate the 5HT2A receptors, so they are not advised (I didn't do well with this supplement) (R).
Even though LSD activates 5HT2A receptors, chronic usage causes a decrease in the number of receptors, which may explain part of the longer term happiness effects (R). Microdosing LSD is something to think about.
Substances That Increase HTR2A
Substances That Decrease HTR2A
Read: 5HT2A Receptors: A Root Cause of Anxiety, Fatigue, Sleep Problems and CIRS
Activation of 5HT2A receptors contributes to:
- Anxiety and neuroticism. In particular, it increases glutamate release and neuronal excitation (R).
- Increased TGF-beta (R) - this effect is reversed by NAC and lipoic acid (R).
- Decreased glutathione (R)
- Reduced BDNF . When activated, these receptors decrease BDNF production (R). This is the mechanism by which psychological stress reduces BDNF (R).
- Increased arachidonic acid, which can be inflammatory (R).
- Suicide and depression. Suicidal and otherwise depressed patients have had more 5-HT2A receptors than normal patients (R). Blocking these receptors is a mechanism of antipsychotics and can help depression (R). This receptor may to some extent account for the difference in the outcome of anti-depressant/SSRI treatment (minor alleles generally more likely to benefit) (R). 5HT2A receptors are in high concentration in the default mode network [DMN], which is overactive in depression (R). This brain network is implicated in self-related thinking and mind wandering.
- Chronic Fatigue Syndrome. One study has linked abnormal 5-HT2A polymorphisms which may enhance receptor activity with Chronic Fatigue Syndrome (R). It's possible that by activating the 5HT2A receptors, fatigue occurs because orexin neurons are shut off. Antipsychotics that block 5HT2A receptors were found to activate orexin neurons (R).
- Insomnia and sleep problems (R).
- IBS . People with genes who produced more 5HT2A receptors were more likely to have IBS (T allele for ) (R). When I took LSD (strong 5HT2A activator), it caused serious GI issues, which fits with this.
- Decreases Slow Wave Sleep (along with 5HT6..... 5-HT1A, 5-HT1B, and 5-HT7 MAOA and serotonin transporters have been implicated in the control of REM sleep) (R).
- OCD. Higher numbers of 5HT2A receptors in the caudate nuclei are associated with OCD (R). Blocking the 5-HT2 receptor has been shown to enhance therapeutic responses to SSRIs in patients with major depression and treatment-refractory obsessive“compulsive disorder (OCD) (R).
- Pain. These receptors are found in the spinal cord regions that control pain (R). Activation of 5-HT2A receptors potentiates pain produced by inflammatory mediators (R).
- Autism. These blockers may also be effective in ameliorating some symptoms associated with autism and other pervasive developmental disorders (R). Autistic people have more 5HT2A receptors (in platelets) (R).
- Tourette's (R) and head twitch response (R).
- Increased prolactin, cortisol and renin (activation of the 5-HT2A in the hypothalamus) (R).
- Decreased blood flow to the heart (R), skin (R) and other places. 5HT2A causes your blood vessels to narrow (vasoconstriction of smooth muscle cells) (R). Decreased blood flow can contribute to people feeling colder.
- Increased platelet clumping (R), which can worsen blood flow and cause heart disease.
Activators of 5HT2A (R):
- Lower heart rate and lower blood pressure (mediated by the vagus nerve) (R, R2).
- Reduce inflammatory effects in several tissues including the heart and gut (especially against TNF-induced inflammation).
- Enhance dopamine in the areas responsible for a higher level of thinking (PFC), which enhances memory and plays a role in attention and learning.
- Reduce pressure in the eye,
- Increase oxytocin and ACTH (activation of the 5-HT2A in the hypothalamus).
The lower heart rate and blood pressure are produced via the inhibition of Rostral Ventrolateral Medulla (RVLM) in the brain stem, which controls the baroreflex (R).
The baroreflex controls blood pressure and people with chronic fatigue often have low blood pressure. These effects could, in part, be mediated by the 5HT2A receptors. Other effects could be as a result of lower orexin activation, as orexin neurons from the hypothalamus stimulate the RVLM (R).
The RVLM is the primary regulator of the fight or flight nervous system, sending excitatory signals to the sympathetic preganglionic neurons in the spinal cord, via reticulospinal tract (R).
In animals, the 5-HT2A receptors increase body heat by causing vasoconstriction in skin (mediated by brainstem) (R).
Conditions with Increased Gene Activity
|Condition||Change (log2fold)||Comparison||Species||Experimental variables||Experiment name|
Conditions with Decreased Gene Activity
|Condition||Change (log2fold)||Comparison||Species||Experimental variables||Experiment name|
The following transcription factors affect gene expression:
Detected in brain cortex (at protein level). Detected in blood platelets.
- 1-(4-Iodo-2,5-Dimethoxyphenyl)Propan-2-Amine Binding
- Drug Binding
- G-Protein Coupled Serotonin Receptor Activity
- Neurotransmitter Receptor Activity
- Serotonin Binding
- Virus Receptor Activity
- Activation Of Phospholipase C Activity
- Adenylate Cyclase-Inhibiting G-Protein Coupled Receptor Signaling Pathway
- Artery Smooth Muscle Contraction
- Behavioral Response To Cocaine
- Cell Death
- Cellular Calcium Ion Homeostasis
- Chemical Synaptic Transmission
- Detection Of Mechanical Stimulus Involved In Sensory Perception Of Pain
- Detection Of Temperature Stimulus Involved In Sensory Perception Of Pain
- Negative Regulation Of Potassium Ion Transport
- Negative Regulation Of Synaptic Transmission, Glutamatergic
- Phosphatidylinositol 3-Kinase Signaling
- Phospholipase C-Activating G-Protein Coupled Receptor Signaling Pathway
- Phospholipase C-Activating Serotonin Receptor Signaling Pathway
- Positive Regulation Of Cell Proliferation
- Positive Regulation Of Erk1 And Erk2 Cascade
- Positive Regulation Of Fat Cell Differentiation
- Positive Regulation Of Glycolytic Process
- Positive Regulation Of Map Kinase Activity
- Positive Regulation Of Peptidyl-Tyrosine Phosphorylation
- Positive Regulation Of Phosphatidylinositol Biosynthetic Process
- Positive Regulation Of Vasoconstriction
- Protein Localization To Cytoskeleton
- Regulation Of Behavior
- Regulation Of Dopamine Secretion
- Regulation Of Hormone Secretion
- Release Of Sequestered Calcium Ion Into Cytosol
- Serotonin Receptor Signaling Pathway
- Temperature Homeostasis
- Urinary Bladder Smooth Muscle Contraction
- Ergoloid Mesylate