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Interesting potentials on Histamine3 receptor ligands.

Here I am.

Today i skipped my venlafaxine and valproic acid dose, unfortunately I didn't sleep much but a nice cup of coffee got me back on the rails. I hope my venlafaxine pause wont affect the experiment, however apart from coffe the i've just smoked a few cigs.

- 4:00pm
I ingested 16x4 betahistine pills. The therapeutic dose is 8/16mg 3 times a day due to it's short half life (3-4h).

- 4:25pm
I start to notice some sorto of awakening feeling, nothing like amphetamine but my motivatin to do things increased, I'm home alone and a bit bored and stressed since i spent an hour fixing my PC but the stress went away pretty fast. I start to feel some sort of slight tinging on my limbs.

- 4:45
Definite increase in blood pressure judging from the veins on my arms, but high blood pressure has never been a prblem for me since i normally have low blood pressure.
Psychologically, there is some nice nootropic feeling much higher than piracetam or aniracetam at high doses. The stimulation is kinda smooth I feel confident and motivated but still i can apreciate calmness, this might be due to the supposed gaba release potentials.
Music is just Fiiiine and I noticed some increased in sex drive which i used to miss during my venlafaxine days, that bothered me but now it's good to hear your dick say 'hello'.

- 5:00pm
The effects are still lasting, as i said before is nothing like the amphetamine boom, but a mild stimulation and psychological motivation, i later went on facebook and wrote commented to all the people i felt like when normally I'cant be bothered to answer to mails and such, in my opinion it truly has some nootropic potentials.
Event with high bood pressure, heart beat seems regular. I noticed some slight pupil dilatation when looking myself in the mirror even with side lights.

- 5:30 (now)
I was a bit bored, i am normally really bored so i decided to clean up my room and fix things here and there since my house is kind of falling apart. I wish I had a friend here with me to speak to to analyze any differences in comunication skills. The slight tingling on my arms is over but im still awake and calm at the same time. i'm now listening to the sounds of the city and contemplating about every single one of them.
I normally don't read a lot of books but as of now i believe my atention would be good enough to get involved in a story and not just wikipedia and such.

I'll be back soon!

Cheers
 
Sorry, this has nothing to do with the subject, but in your original post you wrote,
"reminder, please guys sop injecting cruhed, soaked, microfileterd blbla pills:"

What the hell are blbla pills? And when you say "microfiltered", what do you mean? Do you mean filtered through a micron filter? If so, I'd be quite interested to hear you suffered such a bad infection even after micron filtering your pills. It would be important for the community to know if this is the case (from a harm reduction standpoint) because it seems that the generally held belief at BL is that a micron filtered pill is fairly safe to shoot. If it turns out that you did micron filter your pills and still suffered a terrible infection, I think it would be important for the community to know about this. Thanks-DG
 
daddysgone said:
Sorry, this has nothing to do with the subject, but in your original post you wrote,
"reminder, please guys sop injecting cruhed, soaked, microfileterd blbla pills:"

What the hell are blbla pills? And when you say "microfiltered", what do you mean? Do you mean filtered through a micron filter? If so, I'd be quite interested to hear you suffered such a bad infection even after micron filtering your pills. It would be important for the community to know if this is the case (from a harm reduction standpoint) because it seems that the generally held belief at BL is that a micron filtered pill is fairly safe to shoot. If it turns out that you did micron filter your pills and still suffered a terrible infection, I think it would be important for the community to know about this. Thanks-DG
Click to expand...

LOL! I didnt inject the pills! And i never did!
The infection i got was from an unsterilized injection of a benzodiazepine liquid suspension that missed the vein and infected me with a really badass germ (streptococcus i think). Though by injecting pills the risk is far higher. Still always sterilize your vein and dont use the same syringe twice unless disinfected.
 
/navarone/ said:
LOL! I didnt inject the pills! And i never did!
The infection i got was from an unsterilized injection of a benzodiazepine liquid suspension that missed the vein and infected me with a really badass germ (streptococcus i think). Though by injecting pills the risk is far higher. Still always sterilize your vein and dont use the same syringe twice unless disinfected.
Click to expand...

I did not think you injected the histamine related pills. But in your original post, after saying you got a nasty infection you sad ,":reminder, please guys sop injecting cruhed, soaked, microfileterd blbla pills:"

So it sounds like you were injecting some kind of pills-and I was asking what "blbla pills are".-DG
 
MeDieViL said:
Try it with recreational chemicals.
Click to expand...

I'm doubtfull on that, i get wridside effects from amphetamines and the like after my years of abuse, how to say it, the party times are a bit over for me even if im just 21. I've damaged myself enough so i dont want to risk anyfurther, it's difficult here to find 'clean drugs' what you get in clubs is almost always some cut up laced shit. Amphetamines now make me kind of psychotic and stiff minded, MDMA wouldn't be a wise choice. Before mixing crazy shit id like to get back in shape and out of my antidepressant theraphy.

Anyway what do you suggest I should try it with?


EDIT: MY ONE THOUSAND POST!!!!! HURRAY!!
 
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I might give it a try with LSD and some speed maybe.
After my experience with amphetamines, which changed me deeply, I'm being very carefull.

Anyway it was a good experience by Itself, the downside was that when it came down I felt pretty sleepy but the sleep was incredibly relaxing.
 
1. Venlafaxine and its active (!) metabolite have a t1/2 of 5 resp. 11 hours. Leaving out the venlafaxine for just one day doesn't mean that it is washed out of your system, especially not if you're taking the drug on a regular base and have quasi a steady-state blood-level. If you're taking a retained-release form, it's even worse.
Question: How can we know that there ain't any interactions? Obvious answer: We can't.
Question: What is the whole bioassay worth then? Answer: Nothing. :\

2. Anybody elso here who thinks that it is not the wisest decision to test a new compound when you are already on 2 other drugs? Are you not afraid of any kind of interaction? This is indeed irresponsible and sends the wrong message to other users, who might get encouraged by this behaviour.


@Daddysgone: "blbla" is probably just another typo...


Sorry to say so, but this thread is so depressing. Not that I disagree with the topic per se (H3 as a target is certainly highly interesting), but the level of discussion fluctuates between pointless, sad and hilarious :|

- Murphy
 
Murphy, I'll refrain from numbering my responses since in honest opinion it is a cold way to adress to someone.

You might think that I've just recklessly read an article on wikipedia and felt an orgasmic urge to investigate this neglected and underestimated field of pharmacology by foolishly running to the pharmacy with my 'prescription' and later running home with a delirious looking face craving to intoxicate my self irresponsably without consulting any reliable source of information.

Sorry to disprove your stand but I have done my homework.
I've read extensively all the information booklets and consulted wikipedia regarding any kind of interaction, also i've specifically googled for interactions between betahistine and venlafaxine and its metabolite (desvenlafaxine) now marketed as Pristiq 'the new effexor'.
I've been on venlafaxine 37.5mg twice daily for no more than a week and yes I'm fully aware of the short half life of its original molecule and the long half life of the parent metabolite and I doubt I would experience any significant withdrawal effects from venlafaxine in such small doses after just a week of treatment.
As for valproic acid, if you know what it is, I haven't found 'any interactions with that as well. Valproate is a GABA transaminase inhibitor as well as a weak Na-Ca voltage-gated channel blocker with a fairly long half life (9-16h) but apart from it's GABA enriching effects and it's ion channel anticonvulsant activity, it's effects on the whole neurotransmitting system is negligible. I was prescribed to it as a 'mood stabilizer' prior to being prescribed to venlafaxine and also because of a couple of seizures due to a sudden benzodiazepine discontinuation that happend almost a year ago.

I forgot to say that I didnt take the valproic acid for 2 days since I forgot to take it with me while i was away from home.
I forgot to point out that I have a very high metabolism and tend sober up a bit quicker than some fo my friends, I also urinate very frequently due to my high consumption of water as a 'body washing' habbit ('the more you pee the better it is' and no my kidneys are fine).
I took the last 37,5mg venlafaxine pill in the morning and started the betahistine experiment the next day at noon.

The only interaction notice i found on the betahistine information booklet was: As of today no interactions have been found between betahistine and other pharmaceuticals, it is although posible that betahistidine might interact with regular antihistamines (the H1-2 ones) normally used to treat allergies or sea-sickness.

Sure it would have been more accurate if i hadn't been taken effexor the days before but from my POV your opinion about my experiment was way too drammatic!

So as far as the information goes I guess I've done my deal of research before doing anything irresposable and gave also a great deal of contribution to this thred by posting all the information I could find including that extensive NCBI-PubMed study.
As for my experiment, I guess that has done some contribution to this study and I would like to try it again but for now I don't want to neglect my effexor theraphy.

Now before finishing my post I would honestly like to deal with something off topic.
It has come to my unfortunate attention that you seem to be irritated by my presence on this discussion board. Sure I'm no genius and yes I've posted some nonsense and a lot of typos, I've always respected you as it is evident that you're knowledge on the matter is indeed profound, however without being arrogant you've seem a bit harsh on your posts and more prone to criticize rather than giving a humble opinion.
This adversion saddens me slightly and I hope that your scientific criticism doesn't become a personal hardship.
So far your posts on this thread have expressed a derision towards my thread but still stating that H3 receptor actvity is an interesting subject. I would be glad to see some your contribution on this subject so I humbly invite you to share some of your words on the matter that you define interesting rather that bashing what has been done so far.

I hope this will settle the waters.

Peace
 
Found this patent on the antidepressant potentials of betahistine, faily long but a few chapters a very interesting.

Treatment Methods Employing Histamine H3 Receptor Antagonists, Including Betahistine.

Abstract:
Methods of treating depression, binge eating disorder, narcolepsy, excessive daytime sleepiness, substance use disorders, and Prader Willi syndrome, disorders characterized at least in part by hypocortisolemia and decreased activity of the hypothalamic-pituitary-adrenal (HPA) axis, and disorders related to disturbances in circadian rhythm, comprising the step of administering an effective amount of a histamine type 3 (Bb) receptor antagonist, such as betahistine or its pharmaceutically acceptable salts, or its metabolites to an individual.

Claims:
1. A method of treating depression comprising the step of administering an effective amount of an (H.sub.3) receptor antagonist to an individual in need thereof.

2. The method according to claim 1, wherein the H.sub.3 receptor antagonist comprises betahistine or a pharmaceutically acceptable salts thereof.

3. The method according to claim 1, wherein the H.sub.3 receptor antagonist comprises betahistine hydrochloride or betahistine mesylate.

4. The method according to claim 1, wherein the H.sub.3 receptor antagonist comprises at least one metabolite of betahistine or a pharmaceutically acceptable salt thereof.

5. A method according to claim 1, wherein depression comprises an atypical subtype of depression.

6. The method according to claim 5, wherein "treating" comprises treating at least one symptom associated with the atypical subtype of depression, wherein the at least one symptom is selected from the group consisting of fatigue, hypersomnia and increased appetite/weight gain.

7. The method according to claim 1 wherein the depression comprises bipolar depression.

8. The method according to claim 1, wherein an effective amount comprises a dosage of at least about 48 mg per day.

9. The method according to claim 8, wherein the dosage is administered orally.

10. The method according to claim 9 wherein the effective amount comprises a dosage of between about 48 mg per day and about 480 mg per day.

11. The method according to claim 10 wherein the effective amount comprises a dosage of about 96 mg/day.

12. A method for treating a patient suffering from, recovering from, or predisposed to, one or more disorders selected from binge eating disorder, narcolepsy, excessive daytime sleepiness, substance use disorders, and Prader Willi syndrome, the method comprising: administration of an H.sub.3 antagonist to the patient.

13. The method according to claim 12, wherein the substance abuse disorder comprises alcohol abuse.

14. The method according to claim 12, wherein the H.sub.3 antagonist comprises betahistine or a pharmaceutically acceptable salt thereof.

15. A method for treating patients suffering from disorders characterized at least in part by hypocortisolemia and decreased activity of the hypothalamic-pituitary-adrenal (HPA) axis, comprising administration of an effective amount of an H.sub.3 antagonist to the patient.

16. The method according to claim 15, wherein the disorder is selected from post traumatic stress disorder, fibromyalgia, chronic fatigue syndrome, somatoform pain disorder, multiple sclerosis, and rheumatoid arthritis.

17. The method according to claim 15, wherein the H.sub.3 antagonist comprises betahistine or a pharmaceutically acceptable salt thereof.

18. A method of adjusting a circadian rhythm disturbance in an individual comprising administration of an H.sub.3 antagonist.

19. The method according to claim 18 wherein the individual suffers from seasonal affective disorder.

20. The method according to claim 17, wherein the H3 antagonist comprises betahistine or a pharmaceutically acceptable salt thereof.
 
(WO/2007/076140) TREATMENT METHODS EMPLOYING HISTAMINE H3 RECEPTOR ANTAGONISTS, INCLUDING BETAHISTINE

This similar patent about the neuronal effects of betahistine states further down something a bit dissapointing about the bioavailability of the compound.
It seems that regardless of the incredible low toxicity and drug adverese reactions ( Betahistine : A retrospective synopsis of safety data by S. Jeck-Thole & W. Wagner ,Solvay Pharmaceuticals) of betahistine even at doses as high as 300mg a day, the drug is metabolized tremendously fast into it's inactive metabolites by the liver thus only about 1% (IIRC) of the compound crosses the blood-brain barrier to exert it's beneficial neuropharmacological properties.
There are some debates on which salt (currently HCl and mesylate) or which prodrug formulation would overcome this unconvenience thus redeucing the dose of administration and dose dependet toxicity.
It has been also found that minor active metabolites are produced in vivo but their efficacy as compared to the parent compound is yet to be seen.

Still more than one study has shown to be an beneficial drug in the trreatment of different forms of depression and dementia by its ability to release and regulate plurious neurotrasmitters thus increasing motor function, modulating brain reward system, and improve cognitive functions.

As MeDieVil posted above there is a very brief chapter referring to other studies regarding the potentials of histamine activity in the rewards mechanism of some common drugs of abuse like methamphetamine cocaine and opioids.
 
http://dmd.aspetjournals.org/content/2/2/123.abstract

There might be a Possible way to overcome the problem caused by the fast degradation of betahistidine before reaching the brain.
It seems that the main metabolism process which degrades betahistidine almost completely is done my MAO, turning it into 2-pyridylaceticacid, also trance amount of the demethylated drug was found. It was revealed that betahistidine has greater affinity for mitochondril MAO than tyramine, serotonin and benzylamine.
 
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Common guys lets stay ontopic.
Navarone's spelling mistakes are quite funny but no need to completely waste a topic that could be pretty interesting.
 
OOOh please excuse me for my spelling mistakes, unfortunately English isn't my mother toungue and I've been learning it for only 4 years. And from my POV I'm pretty satisfied with my results since I speak 4 different laguages. Plus my keyboard fucks up once in a while.

MeDieVil...BTW did you get the chance to betahistidine yet? 64mg where pretty low for me but I did notice some interesting effects. Let us know how it goes with you.

Peace.
 
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I havent tried it yet, but i'm planning to get it prescribed because a good bioassay of this compound would requre dosing a few days. Its not a recreational drug and needs longer trialling.
 
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