Talk:5-HT7 receptor

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"The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature and in the gastrointestinal tract.[1]... The 5-HT7 receptor is involved in thermoregulation, circadian rhythm, learning and memory, and sleep. "

How is the effect of this receptor when agonized or antagonized. Smooth muscle is relaxed when receptor is agonized or antagonized? Anybody knows it? And the same i wanna know when it comes about termoregulation, memory etc.

Im takins amisulpride 50-100mg. This drug antagonize 5ht7a. I have no problem sleeping, learning and good memory. So probalby antagonizm of 5ht7a improve these things.

I also have problems with cold hands (shrinked vessels) especiali in the mornings and gastrointestinal tract. It could be becouse of i am nervous, anxiety, depresed etc but im knot sure of amisulpride's involvment at this. Recently i also have a little bit elevated body temperature for long time (sometime is normal somethimes not). And im knot sure if it is some kind of infections or maybe amisulpiride and it's 5ht7a antagonism... — Preceding unsigned comment added by 109.241.248.66 (talk) 14:40, 22 October 2014 (UTC)[reply]

Welcome to Wikipedia! Please note that we cannot offer medical advice here. Your first questions (regarding activation / antagonism of the receptor) could probably be asked at [1], but also there specific medical advice is off-topic. Please discuss your specific case and side effects with a doctor. MichaK (talk) 17:47, 22 October 2014 (UTC)[reply]

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The list of “Antagonists” and “Inverse Agonists” under section 4 (Ligands) is a bit misleading. This article defines an antagonist as a ligand that binds the receptor but has not effect of its own and occludes the binding of agonists/inverse agonists only; however, the appropriate term for this is “Neutral Antagonist.” The majority of antagonists tested for the inhibition of constitutive 5-HT7 activity display marked inverse agonism. I am only aware of 3 drugs (methysergide, metergoline, and mesulergine) that are neutral antagonists at the 5-HT7(a) receptor. This brings up another issue about this section – inverse agonist efficacies differ between the three human splice variants (Krobert et al. 2002). In this case, we would have to define the neutral antagonists and inverse agonists for each receptor splice variant. The simpler approach is to merge the “Antagonist” and “Inverse Agonist” section into one section called “Antagonists.” Otherwise, the structure of this section of the article may become very clumsy and difficult to understand for more lay audiences. As far as the discrepancy between “inactivating antagonists” and “desensitizing antagonists” – the issue pertains to the unique mechanism of action of these antagonists at the 5-HT7 receptor. Receptor desensitization is classically described by agonist stimulation of a receptor followed by phosphorylation, recruitment of beta-arrestin, and receptor internalization. The 5-HT7 receptor does not show a significant degree of internalization when exposed to agonists and no internalization when exposed to antagonists (Smith et al. 2006). Thus the tern “inactivating antagonists” has been adopted to the class of drugs that bind the 5-HT7 receptor and prevent stimulation by agonist, presumably via an irreversible/pseudo-irreversible interaction between antagonist and receptor. Radiolabeled risperidone (one of the six inactivators) has been shown to irreversibly bind to the h5-HT7 receptor, and it is presumed that the other inactivates produce there effects by a similar mechanism.

Last edited at 21:05, 24 July 2009 (UTC). Substituted at 06:09, 29 April 2016 (UTC)

Why don't I see anything about the affinity this receptor has for psychedelic compounds?

Following the work of Thomas Ray I am intrigued by the effects the 5-HT7 receptor is supposed to have: https://transformpress.com/images/Downloads/S02Methods.pdf. I am wondering why I don't see anything about this research on this page. Is it because these effects are still deemed to speculative? — Preceding unsigned comment added by 77.251.116.230 (talk) 11:46, 11 January 2022 (UTC)[reply]