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Serotonin 5-HT(1)A Receptor and Male Sexual Function / Motivation

serotonin 5-ht1a receptor male sexual function motivation libido agonist antagonist pssd cure

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#91 dramachiavellian

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Posted 26 March 2018 - 05:50 PM

https://www.ncbi.nlm...pubmed/15951399

 

 

Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties.
Abstract

Recent data has suggested that the 5-hydroxytryptamine (5-HT)(1A) receptor is involved in cognitive processing. A novel 5-HT(1A) receptor antagonist, 4-cyano-N-{2R-[4-(2,3-dihydrobenzo[1,4]-dioxin-5-yl)-piperazin-1-yl]-propyl}-N-pyridin-2-yl-benzamide HCl (lecozotan), which has been characterized in multiple in vitro and in vivo pharmacological assays as a drug to treat cognitive dysfunction, is reported. In vitro binding and intrinsic activity determinations demonstrated that lecozotan is a potent and selective 5-HT(1A) receptor antagonist. Using in vivo microdialysis, lecozotan (0.3 mg/kg s.c.) antagonized the decrease in hippocampal extracellular 5-HT induced by a challenge dose (0.3 mg/kg s.c.) of 8-hydroxy-2-dipropylaminotetralin (8-OH-DPAT) and had no effects alone at doses 10-fold higher. Lecozotan significantly potentiated the potassium chloride-stimulated release of glutamate and acetylcholine in the dentate gyrus of the hippocampus. Chronic administration of lecozotan did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model indicative of 5-HT(1A) receptor function. In drug discrimination studies, lecozotan (0.01-1 mg/kg i.m.) did not substitute for 8-OH-DPAT and produced a dose-related blockade of the 5-HT(1A) agonist discriminative stimulus cue. In aged rhesus monkeys, lecozotan produced a significant improvement in task performance efficiency at an optimal dose (1 mg/kg p.o.). Learning deficits induced by the glutamatergic antagonist MK-801 [(-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate] (assessed by perceptually complex and visual spatial discrimination) and by specific cholinergic lesions of the hippocampus (assessed by visual spatial discrimination) were reversed by lecozotan (2 mg/kg i.m.) in marmosets. The heterosynaptic nature of the effects of lecozotan imbues this compound with a novel mechanism of action directed at the biochemical pathologies underlying cognitive loss in Alzheimer's disease.

 

the study is a little off topic, but there are selective 5ht1a antagonists out there and they appear to be nootropic in nature. lecozotan's finished one of its phase 3 trials according to wikipedia, would be interesting to see if increased libido is listed as a side effect

 



#92 magniloquentc0unt

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Posted 08 May 2018 - 06:37 PM

yeah well how come vortioxetine is marketed as procognitive and even named BRINTELLIX (intell as intelligence)... its mainly a 5ht1a agonist.... meh go tell!

anyway, ive been investigating the 5ht1a receptor to address my delayed ejactulation and ive found the following: 

 

Accordingly, in rats, 8-OH-DPAT [5ht1a agonist] produces a dramatic decrease in the ejaculation latency and the number of mounts and intromissions preceding ejaculation (Ahlenius et al., 1981Hillegaart & Ahlenius, 1998Hillegaart et al., 1991). 



#93 magniloquentc0unt

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Posted 14 May 2018 - 06:38 PM

yeah well how come vortioxetine is marketed as procognitive and even named BRINTELLIX (intell as intelligence)... its mainly a 5ht1a agonist.... meh go tell!

anyway, ive been investigating the 5ht1a receptor to address my delayed ejactulation and ive found the following: 

 

Accordingly, in rats, 8-OH-DPAT [5ht1a agonist] produces a dramatic decrease in the ejaculation latency and the number of mounts and intromissions preceding ejaculation (Ahlenius et al., 1981Hillegaart & Ahlenius, 1998Hillegaart et al., 1991). 

 

although this is fairly contrary to my personal experience with vortioxetine....

any toughts on metergoline anyone?



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#94 agwoodliffe

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Posted 21 July 2018 - 11:29 AM

In case this hasn't been mentioned already, I have 1 study here that throws a spanner in the theory that 5-ht1a has a negative effect on sexual functioning. For those who can't be bothered to read it, the study compares 4 beta blockers on rat sexual functioning. The drugs used were atenolol, labetalol, propranolol and pindolol.

The latter 2 were found to have profound negative effects on sexual functioning. The authors proposed that this effect was due to their antagonistic activity at 5-ht1a receptors.

 

https://www.scienced...09130579090065P





Also tagged with one or more of these keywords: serotonin, 5-ht1a receptor, male sexual function, motivation, libido, agonist, antagonist, pssd cure

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