SSRI blocks Muscarinic acetylcholine receptors, could lead to sexual dysfunction

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quagmire
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SSRI blocks Muscarinic acetylcholine receptors, could lead to sexual dysfunction

Unread post by quagmire »

SSRI blocks(antagonist) Muscarinic acetylcholine receptors. It seems that blocking of mACh-receptors could lead to sexual dysfunction.


Values are Ki (nM). The smaller the value, the more strongly the drug binds to the Muscarinic acetylcholine receptor.

(M1-M5)= Muscarinic acetylcholine receptor 1-5

ND = No data

mACh = Muscarinic acetylcholine receptor, not specified M1-M5.



Sertraline: mACh Ki (nM) 427–2,100

Mirtazapine mACh Ki (nM) 670

Ecitalopram mACh Ki (nM) 1,240

Citalopram M1 Ki (nM) 1430

Fluoxetine M1 Ki (nM) 870
M2 Ki (nM) 2700
M3 Ki (nM) 1000
M4 Ki (nM) 2900
M5 Ki (nM) 2700

Paroxetine M1 Ki (nM) 72
M2 Ki (nM) 340
M3 Ki (nM) 80
M4 Ki (nM) 320
M5 Ki (nM) 650



Quetiapine(Antiphsychotic)

M1 Ki (nM) 858 Antagonist
M2 Ki (nM) 1,339 ND
M3 Ki (nM) >10,000 Antagonist
M4 Ki (nM) 542 ND
M5 Ki (nM) 1,942 Antagonist



"Segraves proposed that cholinergic potentiating of adrenergic activity may be primarily
responsible for bethanechol-induced reversal of SSRI-induced sexual dysfunction."
https://www.mdedge.com/psychiatry/artic ... ysfunction

"For example, at
high dosages paroxetine is believed to block
norepinephrine reuptake, and it has a clinically significant anticholinergic effect"
https://mdedge-files-live.s3.us-east-2. ... ticle1.pdf


Role of acetylcholine in control of sexual behavior of male and female mammals.
https://www.ncbi.nlm.nih.gov/pubmed/24561063

Acetylcholine as a Possible Neurotransmitter in Penile Erection
https://core.ac.uk/download/pdf/12170112.pdf

Muscarinic and nicotinic influences on masculine sexual behavior in rats: Effects of oxotremorine, scopolamine, and nicotine
https://www.sciencedirect.com/science/a ... 579390024N

Current drug use as risk factor for erectile dysfunction: results from an Italian epidemiological study.
"In conclusion, after taking account of related pathologies,
our results suggest that men treated with antipsychotic, diuretic and anticholinergic drugs are at greater risk of ED."
https://www.ncbi.nlm.nih.gov/pubmed/12904809


"The sympathetic neurons play the predominant role in the ejaculation process. Their nerve terminals secrete primarily norepinephrine,
although other neurotransmitters such as acetylcholine and nonadrenergic/noncholinergic also play important roles."
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4896089/



""With introduction of acetylcholine(one of the major neurotransmitters) directly into the septal region" the authors reported,"the patient
became euphoric (often experiencing sexual orgasm)"
The Science of Orgasm
By Barry R. Komisaruk, Carlos Beyer-Flores, Beverly Whipple
https://books.google.no/books?id=2As5NR ... ne&f=false
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kpavel
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Re: SSRI blocks Muscarinic acetylcholine receptors, could lead to sexual dysfunction

Unread post by kpavel »

What I like about SSRIs is their 'selectiveness', meaning you have to look for their dirty action in every corner of pubmed.
finities infinities
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Re: SSRI blocks Muscarinic acetylcholine receptors, could lead to sexual dysfunction

Unread post by finities infinities »

Postsynaptic 5ht1a receptor decrease acetylcholine and glutamate in hippocampus- maybe is do you mean?
Muscarinic receptor is antidopaminergic, muscarinic antagonist disinhibition dopamine.
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