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Non-Stimulant Anorectants

Hammilton

Hammilton

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Sep 2, 2008
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I've been dong some reading about non-stimulant anorectants, and what I've found is quite interesting.

Clin Exp Pharmacol Physiol. 1979 Jan-Feb;6(1):81-6

Anorectic and motor activity effects of some 1-benzylcycloalkylamines in the rat.

Mrongovius RI, Ghosh P, Bolt AG.
A series of 1-benzylcycloalkylamines with cycloalkyl rings of five, six or seven carbons and with various benzyl ring substituents (3-Cl, 4-Cl, 4-F, 3-CF3) was prepared and tested for anorectic and motor activity effects in rats. 2. Two potent, non-stimulant, anorectics were found: 1-(3-chlorobenzyl)-cycloheptylamine, and its N-methyl analogue. The activity of these compounds resembled that of chlorphentermine.

PMID: 761429 [PubMed - indexed for MEDLINE]
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Is anyone here aware of how strong a 5HT releaser these compounds are?

Interesting structures, too; I hadn't seen any phentermine derivatives with the alpha-dimethyl groups turned into rings before. It's amazing how many derivatives of one very simple structure you can get, actually. Even more amazing is that so many of them retain activity.

I can't wait to see someone suggest (7S)-7-benzylbicyclo[2.2.1]heptan-7-amine in the SOTF thread. 8) lol
 
Forgive my ignorance, but please define anorectics. I know anorectics and anorexics but I am not familiar with this term.
 
Here is one:

jm00157a601.fp.png
 
That's an interesting structure! Everything I've been finding on the subject seems to be 5HT releasers, with 5HT2b agonist properties that make them a. neurotoxic and b. cardiotoxic.

Since this doesn't block monoamine reuptake or increase release, I'm left wondering how exactly it does so. I assume it does so centrally.

My first thought is CB1 antagonism, but that seems unlikely.
 
it doesn't have to interact directly with any neurotransmitter system
perhaps it could just screw with the hypothalamus, for example increasing the ATP turnover in the hypothalamus interferes with the perception of hunger.
or it could act peripherally and effect the pancreas?? or it can speed up metabolism?
 
Well certainly, but I'm not aware of any drugs with similar activities that look similarly structurally. Though not really something I've paid much attention to.
 
I'm betting that the compound described (number 3) still has some ability to inhibit the noradrenaline transporter (NET), even if it was not readily detected by a 1980s-era synaptosomal uptake assay. It could also be a 5-HT2C receptor agonist. Selective 5-HT2C agonists have a non-stimulant (even stimulant-attenuating) profile and are potent anorectics.
 
^Got in before me, i was thinking of cyproheptadine being an appetite stimulant, and it is a 5ht2c antagonist.

http://en.wikipedia.org/wiki/YM-348 - Here's an agonist.

http://en.wikipedia.org/wiki/RS-102,221 - And a potent antagonist.. interesting that it modulates the dopamine system.

It has anxiolytic effects in animal studies,[2] increases the effectiveness of SSRI antidepressants,[3] and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT2C receptor in regulation of the dopamine signalling system in the brain.[4][5][6][7]
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Wow, RS-102,221 seems like it'd have to be super expensive. I don't see that on the RC market anytime soon.
 
Simmondsin?

The vagus nerve is involved in the anorexigenic effect of simmondsin in the rat.

Flo G, Van Boven M, Vermaut S, Daenens P, Decuypere E, Cokelaere M.
Interdisciplinary Research Centre, Katholieke Universiteit Leuven, Belgium.
Simmondsin, 2-(cyanomethylene)-3 hydroxy 4,5 dimethoxy cyclohexyl beta-D-glucoside, from jojoba meal reduces food intake in rats. We investigated the mechanism of action simmondsin, by studying the effects of fasting or of vagotomy on the food intake reduction. The food intake reduction was significantly less in fasted rats than in non-fasted rats. The reduction of food intake was also significantly diminished after vagotomy. The results of the present experiments suggest that simmondsin reduces intake of food in rats through the augmentation of satiety, in part vagally mediated. Copyright 2000 Academic Press.
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thanks for that hamhurricane.

i do actually have some rimonabant though not taking it atm and did not stick it out for very long as i did not find it to be of much use. another one i have that is used off-lable for weight loss is betahistine hydrochloride. also think i might have some clenbuterol and t3 thyroid hormone somewhere as well..... And i have a few pseudoephadrine tablets which i bought for weight loss. I am not taking all these at once of course.

i am currently on phentermine for weight loss and i am taking some metformin for good measure. i know you will probably think i should just do some exercise but i do and try to eat right but find it hard to lose weight. does not help that i do binge eat on occassions which i try to control.

i guess my question is out of all the supposed weight loss gear that i have, which would be best and what combinations could i use? i understand clen and t3 can be stacked together but i find the side effects too much and i worry what it will do to my thyroid hormones long term.

i know i am crazy and ocd about it but i appreciate any knowledge you could share.
 
I need to lose a fair bit, negrogesic - at least 30 kg (66 lbs). I have lost around 2 kg in the past month. I do need to exercise more which I am doing but I just need some help with the psychological side to help with food choices.
 
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