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Interesting potentials on Histamine3 receptor ligands.

/navarone/

/navarone/

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Interesting potentials on Histamine3 receptor activity

Heya fells!

sory fo not having ben n the DB for so log but i was hospitlized for 16 daysdue to a severe mucle infection, they mutilated my arm to ger rid of thehat nasty infection but eiteir that or amputation.
:reminder, please guys sop injecting cruhed, soaked, microfileterd blbla pills:

Neways back on topic: i'm a bit sleepy right now so im not gonna make this long but i'll put a few references that i tought where rather intersting.
It seems that Histaminic[H3] receptor is cabable of modulation the release of
both GABA, dopamine, noradrenaline, acetylcholine and serotonin. Glutamate seems a recent one)

However i still dont get if its agonist or antagonist that improve/or decrease the realease of theese neurotransmiters.

Studies on theese kind of compounds may help some coditons like obesity,skizophrenia, ADHD, movement disorders and possibly...depressons.
Further intesive studies are still on the go.

NOTE:Most of the info above come from Wikipedia
Histamine_H3_receptor
But there are plenty of RC worth to talke a look.

I would be super duper happy if murphy, hammy, F&B could share their divine kowlegnde on this.

PS: has anyonelse here ever tried a selective H3 ligand?

Regards
 
Last edited:
/navarone/ said:
Heya fells!

sory fo not having ben n the DB for so log but i was hospitlized for 16 daysdue to a severe mucle infection, they mutilated my arm to ger rid of thehat nasty infection but eiteir that or amputation.
:reminder, please guys sop injecting cruhed, soaked, microfileterd blbla pills:

Neways back on topic: i'm a bit sleepy right now so im not gonna make this long but i'll put a few references that i tought where rather intersting.
It seems that Histaminic[H3] receptor is cabable of modulation the release of
both GABA, dopamine, noradrenaline, acetylcholine and serotonin. Glutamate seems a recent one)

However i still dont get if its agonist or antagonist that improve/or decrease the realease of theese neurotransmiters.

Studies on theese kind of compounds may help some coditons like obesity,skizophrenia, ADHD, movement disorders and possibly...depressons.
Further intesive studies are still on the go.

NOTE:Most of the info above come from Wikipedia
Histamine_H3_receptor
But there are plenty of RC worth to talke a look.

I would be super duper happy if murphy, hammy, F&B could share their divine kowlegnde on this.

PS: has anyonelse here ever tried a selective H3 ligand?

Regards
Click to expand...
I took the time and marked all typos in your post in red. :\
Well, maybe FnB, your buddy Hammi and Murphy are not really up to reply to this sick joke. :|

At least for my part I can confirm that my knowledge is neither divine nor that I know anything about H3-receptors further than what is already written at Wikipedia. Not joking here. You should better get clear-thinking before spamming the forum with such nonsense. It's not the first time ... :(

Enough...


- Murphy
 
I apolagise for the typos, as I said was a bit tired and my keyboard is really unconfortable.

However, I don't quite understand why you see this thread as a "spam of nonsense" or sick joke. I would thank you if you could explain this to me.

I obviously read this on wikipedia, and was intrigued by the potentials of this receptors in regulating other neurotransmitters level unlike other histamine receptors.
Also from what i read it seems that this receptor was not taken much in consideration until recently since some research drugs are being developed to treat some of the conditions I posted above.
To me, it seemed interesting and worth investigating/discussing about it.....
I has hoping to gather some more infor from you.

Could you be so kind to highlight the stupidity of my 'spamming' thread please?
 
Because you're posting in such a way that anyone who could possibly reply would be willing to do so due to the shear difficulty of getting through the crap. It's sad that a german is correcting your english spelling. That should be my job :)

Either you need to take the time and get basic spelling correct or post some time when you can devote the effort. Write it out in Word even. I've still not bothered to have internet installed at home so whenever I get a good idea, I that's what I do. I find I put more effort if I'm writing it out a day in advance.
 
onmyway said:
lately i have been interested in histamine antagonists. apparently histamine does have some role in inhibiting the dopamine release involved in reward pathways. i discovered this when i was trying to figure out why people mix seroquel with cocaine.

i havent had time to really dig into this, but i think there is something interesting going on with histamine and dopamine.

Endogenous histamine inhibits the development of morphine-induced conditioned place preference
Click to expand...

Seroquel with coke? WTF? That would completely ruin the experience.
 
Thioperamide, the selective histamine H3 receptor antagonist, attenuates stimulant-induced locomotor activity in the mouse.
Clapham J, Kilpatrick GJ.

Department of Pharmacology (2), Glaxo Research & Development Ltd., Ware, Herts., UK.
The effects of the selective histamine H3 receptor agonist (R)-alpha-methylhistamine and antagonist thioperamide on stimulant-induced locomotor activity in the mouse were examined. Amphetamine (1 mg.kg-1 s.c.), apomorphine (2 mg.kg-1 s.c.) or cocaine (5 mg.kg-1 s.c.) increased locomotor activity. Neither thioperamide (10 mg.kg-1 i.p.) nor (R)-alpha-methylhistamine (20 mg.kg-1 i.p.) affected spontaneous locomotor activity in their own right. (R)-alpha-Methylhistamine (0.3, 3 or 20 mg.kg-1 i.p.) also had no effect on amphetamine (1 mg.kg-1 s.c.)-induced locomotor activity. In contrast, thioperamide (0.2-10 mg.kg-1 i.p. or 0.3-20 micrograms i.c.v.) inhibited, in a dose-dependent manner, the hyperactivity response induced by amphetamine (1 mg.kg-1 s.c.). (R)-alpha-Methylhistamine (20 mg.kg-1 i.p.) completely reversed the inhibitory response to thioperamide (2 mg.kg-1 i.p.). Thioperamide (2 or 10 mg.kg-1 i.p.) also inhibited apomorphine (2 mg.kg-1 s.c.)- and, to a lesser extent, cocaine (5 mg.kg-1 s.c.)-induced hyperactivity. We therefore conclude that antagonism of the central histamine H3 receptor inhibits, to a varying degree, the effects of locomotor stimulants.
 
Because you're posting in such a way that anyone who could possibly reply would be willing to do so due to the shear difficulty of getting through the crap. It's sad that a german is correcting your english spelling. That should be my job

Either you need to take the time and get basic spelling correct or post some time when you can devote the effort.
Click to expand...

Hammilton, I expect better 'snaps' from you than this. ;) Your job isn't spelling nazi; rather, it's logical and conceptual rigor Nazi. ;)
 
/navarone/ said:
Yah I meant antagonist I got a lil confused sorry.

Betahistine is already on the pharmaceutical market in my country and it doesn't cost shit =D!!

I might be able to give you a experience report really soon people...just gimme the time to talk to someone for a prescription.

Cheers
Click to expand...

Good day folks!

As a man of my word, I returned from my quest to obtain betahistidine (Counterfying prescriptions is my speciality...but shh, let's keep it to ourselfs;)).

BTW, I noticed that the molecule looks surprisingly like phenylethylamine:
220px-Betahistine.svg.png

Quite interesting if you take into account that it could possibly act on DAT or D receptors.

Anyway I just got 20 16mg tablets for less than 10€.
Here it is:
dscn0788z.jpg


I would start the experiment right away but I'm currently under 75mg venlafaxine plus 500 valproic acid daily, so I would prefer to skip my dose for one day and try this compound in complete 'sobriety' in order to get a more accurate observation from this compound.
The therapeutic dose starts from 8mg to 16mg 3 times daily and on the booklet it says that it might take up to 3 days to reach the desired effects, which in their words means diminished vertigo and inhibition of Meniere's disease symptoms.

I'm planning to start with a 16 or even 32mg dose and see what that does.

Be back soon enough with my experience report.
If there's anything you want to tell/advice me, let me know.

Cheers
 
Histamine H3 Receptor Antagonists Potentiate Methamphetamine Self-Administration and Methamphetamine-Induced Accumbal Dopamine Release

interesting, as they seem to have the opposite effect on dopamine release by cocaine.
 
Betahistine is supposed to release neurotrasmitters like dopamine, serotonin, norepinephrine from the dentrites, especially in the vestibular system.
Amphetamines are releasers, cocaine is a reuptake inhibitor for DA 5-HT and NE...that might be the reason.

Did you read the PubMed link I posted above? Lots of info there.
 
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