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Aphrodisiacs of the Future

nuke

nuke

Bluelighter
Joined
Nov 7, 2004
Messages
4,191
Exam season is over so now it's time for some fantastic slacking, how ribald!

What are some good possible aphrodisiacs of the future? 5HT1A agonists facilitate sexual behaviour (among other anxiolytic behaviour) in male rats, but not females.

5-alpha-pregnan-3alpha-ol-20-one analogues may work for females, though:
Infusions of 3alpha,5alpha-THP to the VTA enhance exploratory, anti-anxiety, social, and sexual behavior and increase levels of 3alpha,5alpha-THP in midbrain, hippocampus, diencephalon, and cortex of female rats.
Frye CA, Rhodes ME.

Department of Psychology, University at Albany-SUNY, United States; Department of Biological Sciences, University at Albany-SUNY, United States; Center for Neuroscience Research, University at Albany-SUNY, United States; Center for Life Sciences Research, University at Albany-SUNY, United States.

17beta-Estradiol (E(2)) and progesterone (P(4)) influence the onset and duration of sexual behavior and are also associated with changes in behaviors that may contribute to mating, such as exploration, anxiety, and social behaviors (socio-sexual behaviors). In the midbrain ventral tegmental area (VTA), the P(4) metabolite, 5alpha-pregnan-3alpha-ol-20-one (3alpha,5alpha-THP), modulates lordosis of E(2)-primed rodents; 3alpha,5alpha-THP can also influence anxiety and social behaviors. To examine if 3alpha,5alpha-THP in the VTA mediates socio-sexual behaviors, we infused 3alpha,5alpha-THP to the VTA of diestrous and proestrous rats. As expected, proestrous, compared to diestrous, rats showed more exploratory (open field), anxiolytic (elevated plus maze), pro-social (partner preference, social interaction), and sexual (paced mating) behavior and had increased E(2), P(4), dihydroprogesterone (DHP), and 3alpha,5alpha-THP in serum, midbrain, hippocampus, diencephalon, and cortex. Infusions of 3alpha,5alpha-THP to the VTA, but not control sites, such as the substantia nigra (SN) or central grey (CG), of diestrous rats produced behavioral and endocrine effects akin to that of proestrous rats and increased DHP and 3alpha,5alpha-THP levels in midbrain, hippocampus, and diencephalon. Levels of DHP and 3alpha,5alpha-THP, but neither E(2) nor P(4) concentrations, in midbrain, hippocampus, diencephalon, and/or cortex were positively correlated with socio-sexual behaviors. Thus, 3alpha,5alpha-THP infusions to the VTA, but not SN or CG, can enhance socio-sexual behaviors and increase levels in midbrain, hippocampus, and diencephalon.
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Orexin seems to be implicated in sexual reward, so orexin agonists may lead to fun but as they're mostly peptides administration would be difficult.

The extract of cihuapatli may provide a nice oxytocic effect:
Pro-ejaculatory effect of the aqueous crude extract of cihuapatli (Montanoa tomentosa) in spinal male rats.
Carro-Juárez M, Lobatón I, Benítez O, Espíritu A.

Laboratorio de Comportamiento Reproductivo, Escuela de Medicina Veterinaria y Zootecnia, Universidad Autónoma de Tlaxcala, CP 90000, AP 484, Col. Centro, Tlaxcala, Mexico. [email protected]

In the present study, the pro-sexual effect of the cihuapatli (Montanoa tomentosa) and its possible pro-ejaculatory properties in spinal male rats were examined. Systemic administration of the aqueous crude extracts of Montanoa tomentosa exerted a pro-ejaculatory effect and produced an increase in the number of discharges in the ejaculatory motor patterns in the spinal rats. The cihuapatli-induced ejaculatory responses included the expression of penile erections and penile movements and the potent expulsion of urethral contents and in some cases the expulsion of seminal plugs. The cihuapatli-induced ejaculatory motor patterns were similar to that obtained after systemic oxytocin. Cihuapatli- and oxytocin-induced ejaculatory motor responses and the penile erections and movements were abolished by the pre-treatment with hexamethonium, a selective oxytocin antagonist. Present data show that the cihuapatli extract acts directly at the spinal system in charge of the expression of the ejaculatory motor patterns and suggest that the aqueous crude extract exerts its aphrodisiacs properties by increasing sexual potency acting as an oxytocic agent.
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http://www.ncbi.nlm.nih.gov/sites/e...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
 
Derivatives of Bremelanotide
250px-Bremelanotide_chemical_structure.png


It's be nice to have some small-molecule drugs that are easier to synth than peptide drugs.
There are a variety of targets we can look at. So far, the MC3-R and MC4-R receptors seem to produce the most "real" aprodiasic effect... but as you say 5-HT1A seems to work too.
 
Yes, it's interesting to note that orexin and MCR-3 and MCR-4 isoform deviations can confer an increased risk of obesity too -- like dopamine, it seems that pleasure-related compounds are the same for food as they are for sex.
 
Clove interestingly enough:
Effect of 50% ethanolic extract of Syzygium aromaticum (L.) Merr. & Perry. (clove) on sexual behaviour of normal male rats.
Tajuddin , Ahmad S, Latif A, Qasmi IA.

Department of Ilmul Advia (Unani Pharmacology), Faculty of Unani Medicine, Aligarh Muslim University, Aligarh-202002, India. [email protected]

BACKGROUND: The flower bud of Syzygium aromaticum (L.) Merr. & Perry. (clove) has been used in Unani medicine since ancient times for the treatment of male sexual disorders. The present study is aimed to investigate the effect of 50% ethanolic extract of clove on general mating behaviour, libido, potency along with its likely gastric ulceration and adverse effects on sexually normal male albino rats. METHODS: The suspension of the extract was administered orally at the dose of 100, 250, and 500 mg / kg, to different groups of male rats (n = 6) once a day for seven days. The female albino rats involved in mating were made receptive by hormonal treatment. The general mating behaviour, libido and potency were determined and compared with the standard reference drug sildenafil citrate. The probable gastric ulceration and adverse effects of the extract were also evaluated. RESULTS: Oral administration of the extract significantly increased the Mounting Frequency, Intromission Frequency; Intromission Latency, Erections; Quick Flips, Long Flips as well as aggregate of penile reflexes and caused significant reduction in the Mounting Latency and Post Ejaculatory Interval. The most appreciable effect of the extract was observed at the dose of 500 mg/kg. The test drug was also found to be devoid of any conspicuous gastric ulceration and adverse effects. CONCLUSION: The results indicated that the 50% ethanolic extract of clove produced a significant and sustained increase in the sexual activity of normal male rats, without any conspicuous gastric ulceration and adverse effects. Thus, the resultant aphrodisiac effectivity of the extract lends support to the claims for its traditional usage in sexual disorders.
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http://www.ncbi.nlm.nih.gov/sites/entrez
 
Sweet, that's interesting about clove. Taste like shit, though.

A very interesting topic, Nuke. I'm surprised it's not getting more talk.

bremelanotide sounds great, though. I've always wondered though, how would the law deal with men slipping that into chicks drinks. I mean, they're still able to choose who, but you could sure as hell increase your odds.
 
^ Yeah, it's an interesting one isn't it.
I suspect, given that it would be logically impossible to /allow/ anyone to dose another person without their consent, that it would be very much illegal.
Imagine that, just suddently getting massively horny in a bar. It'd become difficult to trust yourself, you'd never know when the feelings were genuine.
(shit, that's not good)
How detectable are peptide drugs, say, 24 hours after injestion? I'm guessing that they'd be chopped up by peptidases fairly quickly...
 
Can we get a bit of dopamine tweakage in with these, or is it not necessary (?) Pls excuse my ignorance, I'm here to learn.
MattPsy said:
Imagine that, just suddently getting massively horny in a bar. It'd become difficult to trust yourself, you'd never know when the feelings were genuine.
(shit, that's not good)
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It's happened to me at least once with MDPV, and in a grocery store. Strong desire to follow the poor "victim" around, while trying to masturbate discreetly LOL. Resistable, of course (but not that easily).
 
^ AT least with the MDPV (aside from the fact that in your case you knowingly dosed yourself) you'd be able to tell cause you'd feel all speedy and stuff, whereas if you got dosed with Bremelanotide there are no peripheral effects or anything like that... just arousal! ;p
(and, lol, that's pretty funny... but somewhat disturbing as well, haha.)
 
Bremelanotide actually has quite a few side effects, such as facial flushing and nausea. Aside from that, unless a nanoparticle formulation or something is developed, it'd be hard to slip into a drink (it's destroyed by first pass metabolism).

Dopamine plays a big role in sexuality, and increases in it are normal during any given sexual activity. The sexual act is really a combination of many different neurochemical systems.. Endorphins, dopamine, orexin, melanocortin agonists, prolactin, norepinephrine all play a role
 
arousal is a pretty complex thing.

I just realized how short and stupid that sounds. I'm gonna meditate for a bit and then go to bed. nighters!
 
Oh true, hadn't considered that, that's pleasing.
Wasn't aware of those side effects, either.
Again, pleasing.
(Then again it's probably only a matter of time till we see small-molecule MC3-R agonists...)

With dopamine re: sexuality - is it the case that in order for it to cause hypersexuality, you'd have to have at least some libido first? Because it's a "reinforcing" issue?
 
MattPsy said:
^ AT least with the MDPV (aside from the fact that in your case you knowingly dosed yourself) you'd be able to tell cause you'd feel all speedy and stuff, whereas if you got dosed with Bremelanotide there are no peripheral effects or anything like that... just arousal! ;p
(and, lol, that's pretty funny... but somewhat disturbing as well, haha.)
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I'm not so sure... in lower doses, MDPV seems to have very little effect on norepinephrine, maybe none -- it seems to boost feelings of excitement/anticipation (sexual and otherwise) while not being very speedy at all. It's possible someone who was exposed to a chronic low dose might never notice anything different, aside from feeling more energetic (perhaps chalked up to diet/exercise?) and having a significantly boosted sex drive.
 
Do we need aphrodisiacs for men? Additionally, Yohimbe has millions of years of evolution behind it, yes, but evolution was NOT pushing it to become an aphrodisiac. That's just an unrelated effect top the compound's original intention.
 
Not surprising with it being a 5HT1A antagonist... Doubt I'll ever be giving yohimbine a try in this lifetime, I have enough anxiety as it is.
 
I'm not aware of what auxiliary actions yohimbine might have, but I was specifically enlightened by MJ Millan's claim that it is alpha-adrenergic auto-receptor antagonist. See the article I quoted in the other text. Servier has introduced one conflating that activity with SNRI properties. In summary, enhanced antidepressant efficacy with cognition improving abilities. The 5-HT1A agonist buspirone is metabolized to 1-pyrimidinyl-piperazine which is also a potent alpha-adrenergic auto-receptor antagonist.

I included all that babble in my Wikipedia files but ive sort of run out of steam on that short-winded project, for the time being at least.

Also contraceptive which block estrogen synthesis are pro-depressant. Uh, there are some stuff Chinese are taking that increase the odds of having twins. One can only guess that such compounds are pro-sexual, although no controversy shrouds the fact that they increase fertility.
 
I've taken yohimbe a couple of times out of curiosity. The first time it gave me a boner for about 16 hours, during which I couldn't sleep. I also had persistant nausea. My impression was it seemed to be like a stimulant with no euphoria. I remember a couple of years ago reading uncited claims as to it being an MAOI. Is there any truth to this? This is the main reason I stay away from it.
 
It has some MAO inhibitory activity, but it's not very active (1/100th that of the beta-carboline alkaloids in terms of IC50 concn.). Those reports seem to have come from the fact that it's an alpha-2 antagonist (the autoreceptor for noradrenaline) so that taking a stimulant in conjunction produces a similar sort of end result (hypertension etc)
 
fastandbulbous said:
Yohimbine is also capable of inducing horrible anxiety as well , which will kill arousal as surely as the thought of Maggie Thatcher in a porno pose (as me & Mrs f&b found out the hard way - no pun intended - one night)
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eh you had maggie thatcher in a porno pose which ruined the night? or you had yohimbine?
please clarify :-)
 
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