- 06-09-2012, 05:35 PM
Pat I read your blog explaining why NMT wasn't a good fat burner. In that same abstract you referenced, it mentions isopropyloctopamine. I see the new I-force Dexaprine using it and touting it as very effective. There is also thread her on AM about VPX using it and not being DSHEA compliant. All I really care about is if it works at decent dosages. Thanks in advance.
Isopropylnorsynephrine is a stronger lipolytic agent in human adipocytes than synephrine and other amines present in Citrus aurantium.
Mercader J, Wanecq E, Chen J, Carpéné C.
Institut National de la Santé et de la Recherche Médicale (INSERM), U1048, Toulouse, France.
The weight loss observed in consumers of extracts of Citrus aurantium (bitter orange) has been tentatively attributed to the lipolytic and thermogenic effects of the alkaloids abundant in the unripe fruit. Synephrine, octopamine, tyramine, and other alkaloids have been repeatedly identified and quantified in Citrus members of the Rutaceae family or in their extracts incorporated in dietary supplements for weight management. However, there are only scarce reports on their lipolytic action. This study aimed at comparing the acute lipolytic activity of synephrine, octopamine, tyramine, and N-methyltyramine in rat and human adipocytes. Maximal response to the prototypical β-adrenergic agonist isoprenaline was taken as reference in both species. In rat, octopamine was slightly more active than synephrine whiletyramine and N-methyl tyramine did not stimulate-and even inhibited-lipolysis. In human adipocytes, none of these amines stimulated lipolysis when tested up to 10 μg/ml. At higher doses (≥100 μg/ml), tyramine and N-methyl tyramine induced only 20% of the maximal lipolysis and exhibited antilipolytic properties. Synephrine and octopamine were partially stimulatory at high doses. Since synephrine is more abundant than octopamine in C. aurantium, it should be the main responsible for the putative lipolytic action of the extracts claimed to mitigate obesity. Noteworthy, their common isopropyl derivative, isopropylnorsynephrine (also named isopropyloctopamine or betaphrine), was clearly lipolytic: active at 1 μg/ml and reproducing more than 60% of isoprenaline maximal effect in human adipocytes. This compound, not detected in C. aurantium, and which has few reported adverse effects to date, might be useful for in vivo triglyceride breakdown
- 06-09-2012, 06:13 PM
06-09-2012, 06:21 PM
06-09-2012, 06:33 PM
Pretty benign compound. The para hydroxyl precludes any BBB penetration (thus reducing possible neurotoxicity),and the bulky N-alkyl group restricts against alpha agonism (thus negligable/potentially beneficial effects on blood pressure).
The dose required to induce significant lipolysis would be purely speculative, but caffeine would indubitably synergize.
06-09-2012, 06:34 PM
06-09-2012, 06:35 PM
06-11-2012, 08:51 AM
06-11-2012, 08:53 AM
06-11-2012, 12:08 PM
Yeah, it was tested back in the 80's
http://www.ncbi.nlm.nih.gov/pubmed/6306210This compound was a highly beta selective, direct-acting adrenergic agonist, approximately 200- and 440-fold less potent than isoproterenol in cardiac and smooth muscle, respectively. It was nearly a full agonist in both cardiac and smooth muscle without appreciable selectivity for either beta-1 or beta-2 receptors and had no demonstrable beta blocking activity. No alpha adrenergic activity was detectable within the concentration range tested.
06-12-2012, 02:59 PM
Madchemist summarized things concisely and eloquently, but I'd add that the para-hydroxyl group restricts BBB penetration further, suggesting near-complete CNS preclusion (unlike ephedrine). It seems the necessary PO dose for significant fat loss (against isoproterenol) would stimulate NE vesical exchange, likely resulting in strongly positive chronotropy. Ideally I'd compound this with aminophylline in high-MW carrier for transdermal use.
06-21-2012, 02:46 PM
Hmm. Crushed up Dexa.
BTW, who has that formula now, seeing that Matt left Genomyx?
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