Thought i posted this yesterday. Odd
The anabolic catabolic transfor... [J Cachexia Sarcopenia Muscle. 2013] - PubMed - NCBI
Thought i posted this yesterday. Odd
The anabolic catabolic transfor... [J Cachexia Sarcopenia Muscle. 2013] - PubMed - NCBI
Interesting...
I smell a new research chem
It's just one of the enantiomers of pindolol, a common beta blocker.
Very expensive though. Is it doable as a rc? Evolved? You on the case? LolQuote:
Originally Posted by totalflexblog
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I'll post pa's article on it when I'm on a computer, but it should be pretty easy to find
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Found PA's article and a few more studies.
From Patrick Arnold: (Patrick Arnold » Espindolol (S-Pindolol, MT-102))
Advances in understanding and treating cardiac cachexia: highlights from the 5th Cachexia Conference (Advances in understanding and treating cardiac... [Int J Cardiol. 2010] - PubMed - NCBI)Quote:
Espindolol (S-Pindolol, MT-102)
Anabolic drugs are not dead, in fact research to develop new ones are aggressively being pursued to address medical situations such as cancer cachexia (wasting secondary to cancer) and sarcopenia (age related loss of muscle mass). Both of these categories are potentially huge money makers. Amongst the weird drugs that are being proposed for these applications is one that kind of boggles my mind. It is actually a current drug used to treat high blood pressure. Well, I guess you can say HALF of the drug is being developed as an anabolic
The drug I am referring to is called Pindolol, and the “half” that is being developed is S-pindolol. What I mean by that is that Pindolol is what is known as a racemic compound (it exists in a 50/50 ratio of right and left handed isomers) and the drug proposed as an anabolic is S-pindolol (the left handed isomer only). Many drugs are like this and often only one isomer is the active one. Take for example methamphetamine. Its active isomer is the right handed one. The left handed one is weak enough that it is allowed to be sold over the counter as a component of vicks inhalers.
Pindolol is sold to treat high blood pressure and it does so by blocking the effects of adrenaline like compounds on the heart (it’s a beta1 blocker). As such it decreases the force and frequency of heartbeats and thusly blood pressure decreases. Interestingly, pindolol also has agonist effects upon receptors of adrenaline like compounds too, specifically on skeletal muscle (it’s a beta2 agonist). You may be familiar with beta2 agonists such as clenbuterol. They are anabolic
Anyway, this compound (the S-isomer of pindolol which is the isomer that does stuff) is poised to be marketed as an anabolic for cancer cachexia and maybe sarcopenia. Studies have been done that have demonstrated muscle growth in these models. Myostatin has been shown to be suppressed amongst other things, which are effects we know happens with beta2 agonists (at least in the short term). Cool thing is that unlike most beta2 agonists (clen) this has no stimulatory effect on the heart. Not so cool thing is that it actually has a depressive effect on the heart, which means your exercise performance can suffer because your heart won’t beat fast and hard enough to support your efforts (that is if you train like a man)
Anyway, interesting stuff I suppose and expect it to appear on your banned list soon
Quote:
Int J Cardiol. 2010 Oct 29;144(3):347-9. doi: 10.1016/j.ijcard.2010.05.042. Epub 2010 Jun 19.
Advances in understanding and treating cardiac cachexia: highlights from the 5th Cachexia Conference.Advances in understanding and treating cardiac... [Int J Cardiol. 2010] - PubMed - NCBI
von Haehling S, Stepney R, Anker SD.
Abstract
Cardiac cachexia as a terminal stage of chronic heart failure carries a devastating prognosis. This article focuses on novel insights into the pathophysiology and on new treatment approaches to cardiac cachexia. Drugs that have been used in preclinical and clinical studies that may also confer beneficial effects in cardiac cachexia include but are not limited to the type 4 melanocortin receptor antagonist SNT 207979, the appetite promoting synthetic ghrelin SUN11031, the soluble myostatin decoy receptor ActRIIB-Fc, the fast skeletal muscle troponin activating substance CK-2017357, the anti-catabolic/anabolic transforming agent MT-102, the anti-inflammatory agent celecoxib, and testosterone supplementation.
The ACT-ONE trial, a multicentre, randomised, double-blind, placebo-controlled, dose-finding study of the anabolic/catabolic transforming agent, MT-102 in subjects with cachexia related to stage III and IV non-small cell lung cancer and colorectal cancer: study design. (The ACT-ONE trial, a multicentr... [J Cachexia Sarcopenia Muscle. 2011] - PubMed - NCBI)
Quote:
The ACT-ONE trial, a multicentr... [J Cachexia Sarcopenia Muscle. 2011] - PubMed - NCBI
Stewart Coats AJ, Srinivasan V, Surendran J, Chiramana H, Vangipuram SR, Bhatt NN, Jain M, Shah S, Ali IA, Fuang HG, Hassan MZ, Beadle J, Tilson J, Kirwan BA, Anker SD; on behalf of the ACT-ONE Trial Investigators.
Abstract
AIMS: Cachexia, the wasting disorder associated with a wide range of serious illnesses including cancer, is a major cause of morbidity and mortality. There is currently no widely approved therapeutic agent for treating or preventing cancer-associated cachexia. Colorectal cancer and non-small cell lung cancer have relatively high incidences of cachexia, approximately 28% and 34%, respectively. Neurohormonal overactivity has been implicated in the genesis and progression of cachexia and beta receptor antagonism has been proposed as a potential therapy. MT-102, a novel anabolic/catabolic transforming agent, has a multi-functional effect upon three potential pharmacological targets in cancer cachexia, namely reduced catabolism through non-selective β-blockade, reduced fatigue, and thermogenesis through central 5-HT1a antagonism and increased anabolism through partial β-2 receptor agonism.
METHODS: At least 132 male and female patients, aged between 25 and 80 years with a confirmed diagnosis of late-stage non-small cell lung cancer or colorectal cancer, with cachexia will be randomised to either one of the two MT-102 doses or placebo in a 3:1:2 ratio (MT-102 10 mg BD(-1)/MT-102 2.5 mg BD/placebo). Patients will continue on study treatment for maximally 16 weeks. The primary endpoint, to be analysed by assigned treatment group, will be body weight change over 16 weeks. For this endpoint, the study has 85% power (0.05% significance level) to detect per 4-week period a mean change of -0.8 kg in the placebo group and 0 kg in the high-dose MT-102 arm. The first patient was randomised in February 2011 and patient recruitment is expected to continue until mid-2012.
PERSPECTIVE: The ACT-ONE trial is designed to test whether the anabolic/catabolic transforming agent MT-102 will positively impact on the rate of change of body weight in cancer cachexia, thereby evaluating a novel therapeutic strategy in this hitherto poorly treatable condition. A separate ACT-TWO trial will recruit patients who complete the ACT-ONE trial and remain on randomised double-blind medication. Participants in ACT-TWO will be followed for an additional period with a separate primary endpoint.
I talked about this on my podcast a couple weeks ago. It's mildly interesting, but I'm not sure how great it would be in the long run. It's going to mellow you out and decrease workout performance. Stack with craze? :/)
Purely theoretical but couldn't its mellowing/depressive effects on the heart give this compound more use post-workout or end of the day so that it could potentially help with recovery/repair during sleep? Also seems like it could be extra beneficial when utilizing an IF protocol to promote more anti-catabolism in the body during your fast.
Again...purely just speculation....like this is all highly speculated since there isn't enough info but to me it looks like it could potentially shine during PCT as I can't find anything about it affecting hormone levels. Seems to have SARM like selectivity in terms of agonistic effects on skeletal muscle receptors only. Definitely interested in finding out more about this as it could be a safe addition down the road.