Clenbuterol

2022-11-16:

Clenbuterol #

• β2 agonist. There are all kinds of analogues; formoterol has a 10hr half life instead of 36-48. I think clen became the popular one for no real reason.
  • Anti-catabolic. Hence, combining it with T3 is epic, also when you consider the fact T3 upregulates both β1 and β2 Adrenergic Receptors.
• Mechanisms regulating skeletal muscle growth and atrophy
  • Cellular mechanisms underlying temporal changes in skeletal muscle protein synthesis and breakdown during chronic β-adrenoceptor stimulation in mice
    • β2 agonism from clenbuterol etc. increases AKT phosphorylation… this is
    • Reduces Calpain activity.
    • 12-week old mice: 100 μg kg⁻¹ formoterol. +30% CREB phosphorylation, 11-fold increase in PGC-1α on day 1.
  • The Orphan Nuclear Receptor, NOR-1, Is a Target of β-Adrenergic Signaling in Skeletal Muscle
    • β2 agonism increases NOR-1, which represses the Myostatin promoter.
• 80mg of Clen, without prior use, will increase resting calorie burn by 29%, and fat lipolysis (breakdown to fatty acids) by 39%, along with increasing insulin sensitivity and other fat loss enhancing effects https://thinksteroids.com/community/threads/how-long-can-i-take-clen-for.134425376/#post-3290314
• Makes you shake like you have parkinson’s or something. Some people recommend Ephedrine as an alternative. Though Crimes on nootopics got chronic congestion after using too much ephedrine. Brutal.
  • Leo talks about this being the theory that clen increases the BMR back when it was introduced to bodybuilding. In reality, β2→cAMP→transcription of a few genes like Hormone-sensitive lipase and Acetyl-CoA Carboxylase.
  • The tolerance that quickly develops primarily affects the tremors and boosted twitch speed of muscles. This accounts for only a portion of the extra resting calorie burn, and quickly diminishes as you take the same dose. Some users think that’s an indication it’s no longer working, which isn’t accurate
• Depletes the body’s Taurine, especially during the whole cramping phase. This can cause cramping. People generally say 1g/day, but Judas says you should take 4-10g/day.
  • Taurine in adipocytes prevents insulin-mediated H2o2 generation and activates Pka and lipolysis
    • Tau actions on isolated adipocytes augmented those of β-AR agonists. Tau enhances isoproterenol- and Bt 2 cAMP-stimulated lipolysis by increasing cAMP-dependent PKA catalytic activity.
• Liver autophagy through some unknown mechanism. Despite promoting skeletal muscle hypertrophy, etc.
• Cardiac hypertrophy; colagen infiltration into cardiac structures. deboonked? That’s just thanks to chronically high blood pressure and RHR which other things could do

Albuterol (aka Salbutamol/Ventolin) #

• β2 agonist; even more selective than clen.
• ~5-8hr half life.
• Typical dose is 2-4x8mg. (For asthma that is.). I’m confused though tbh: VigorousSteve says maximum 8mg daily, but that might just be clinical usage. There’s “spillover” to β1 and β3 after 8mg though.
  • It will eventually downregulate? But there’s really no tolerance, especially compared to clen.
• The effect of caffeine and albuterol on body composition and metabolic rate
  • 
    • 4mg once a day = ~140mg increase in BMR.
• β2-Adrenergic agonist salbutamol augments hypertrophy in MHCIIa fibers and sprint mean power output but not muscle force during 11 weeks of resistance training in young men
  • Did not change level of myosin heavy chain I isoforms, suggesting it did not increase proportion os slow twitch. It did increase HC-IIx and decrease IIa.

Nebivolol #

• Selective β1 antagonist, but vasodilatory via some β3 agonism→eNOS. ~19 hour half life in slow CYP2D6 metabolizers
  • β3 agonism is lipolytic; Nebivolol solo is a minor fat burner. Reliable to use for appetite suppression, considering its side effect profile.
• Non-negotiable for minimizing the negative side effects of clen/albuterol. Responsible for heart rate increase and a lot/most of the deleterious effects of SNS activation. β1 is still lipolytic and stuff though.
• Crosses the BBB.

Mirabegron #

• Highly selective β3 agonist. Activates Brown Adipose. CYP2D6 inhibitor. Substantially enhances fat loss if you were to combine it with a β2 agonist.
• Pretty damn expensive