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Saturday, December 31, 2016

Does Ketotifen Really "Upregulate" Beta-Adrenergic Receptors...IN MUSCLE?

For years bodybuilding communities have been touting Ketotifen as some 'magic pill' for upregulating the beta-adrenergic-2 receptors. What we commonly refer to as simply 'beta-receptors'. These receptors are proven mediators of metabolic enhancement; fat burning namely.  They allow us to easier reach our goals of getting shredded and defined.

The problem is - we need to make sure we are actually upregulating the beta-receptors in the muscle, just because something ''upregulates'' them in the Lungs, doesn't mean it will do that elsewhere, and to be clear, I'm not saying it doesn't do that. So little spoiler alert, but you want to read the rest of this to get the full picture.

Ketotifen is a second-generation H1-selective antihistamine with second-messenger enhancing properties [1] [2] [3]. The benefits in Asthma have been accounted for as a functional upregulation in beta-adrenergic 'sensitivity' and density [4] [5]. Now let's go over those terms. 
  • An upregulation simply means an increase in the number of receptors [6].
  • An increase in sensitivity / responsiveness simply means the receptors respond better and more efficiently, to natural adrenaline and ligands such as Clenbuterol [7].
  • An increase in density refers to the increase in the number of receptors studied in a given region, or organ, or culture [8] [9]

<Read this Article on Receptor Density/Affinity>

A ligand is simply a substance that is able to fulfill a certain role in science, but specifically it refers a substance occupying a given target receptor.

So now we fulfill the rest of the research.


You bet!

But it does so in a manner that is very variable depending on DOSE USED and duration of use. Ketotifen usually takes about 'a week to get those results in. Beta-receptor upregulation and sensitization would occur after Day 3 in most people. 

The idea behind ketotifen use of course, isn't a new one. It has been done for years and with good results. Some guys wanna make sure its not all in their head though - and I get that.


There were some studies published in 1996 that indicated that Ketotifen caused weight (including muscle) gain, but in HIV-infected individuals and that the weight gain is caused by TNF-alpha reduction/decreases, but that may also lend support to the beta-receptor hypothesis of anabolism. Since beta-agonists characteristically DECREASE TNF-a themselves [10], this may be the direct result of enhancement of the beta-adrenergic mediated effect by Ketotifen. Once an increase in receptors or receptor sensitivity has been established, then even the natural noradrenaline produced by the human body, as well as adrenaline from other sources, including Epi-pens would be more effective in performing its actions.

Although most of the research regarding Ketotifen focused on mast cells and lymphocytes, there have been some small-scale brain/heart research studies which have provided additional evidence for Ketotifen's widespread upregulation of beta-adrenergic receptors [11] [12] [13].

However, the majority of research focuses on the attenuation of beta-receptor desensitization [14] [15] [16]

Many folks have spouted off saying that Ketotifen can upregulate beta-receptors in just or under 6 hours, that is just not true, nothing works that fast, and that's a misconception unfortunately.

Another common misconception is that ''because Ketotifen is an antihistamine, all antihistamines may increase beta-adrenergic-receptors'', yet, Ketotifen is actually the only antihistamine reliably proven to do so. It displays remarkable brain penetration, as noted in these PET studies

Not only that, but also anecdotally, via forum reports, every community would affirm that Benadryl and other 'crap' antihistamines do nothing for muscle or fat loss, if anything, they make you fatter. Ketotifen is what works. It is said again and again, and it does have anabolic effects.

Several other studies have been conducted since 2006, and some of the newer human studies with Ketotifen have also reinforced the beta-adrenergic modulating actions of this drug [17] [18] [19]. It remains in clinical use for Asthma in most countries, though it is (sadly) withdrawn from the U.S market, it can still be ordered by an Allergist through a compounding pharmacy. A general Doc should also be able to do this, if he is willing [20] [21] [22].

Everything here seems to support the consensus that Ketotifen upregulates beta-adrenergic receptors all throughout the body, but more research needs to be conducted on muscle-related and anabolism related disorders. That is to reach a sensible conclusion that Ketotifen is indeed a non-selective but muscle-acting anabolic agent - through beta-receptor-sparing and upregulating activities [23]. The profile of the medication is elucidated more when viewing the National Library of Medicine's page through the NIH.


Br J Clin Pharmacol. 1995 Feb; 39(2): 109–118.

Curr Opin Clin Nutr Metab Care. 2009 Nov;12(6):601-6. doi: 10.1097/MCO.0b013e3283318a25.

Feng Qing, Christopher G. Rhodes, Michael J. Hayes, Thomas Krausz, S. William Fountain, Terry Jones and J.M.B. Hughes
MRC Clinical Sciences Center, Cyclotron Unit, and Departments of Medicine (Respiratory Division) and Histopathology,
Royal Postgraduate Medical School, Hammersmith Hospital, London, United Kingdom; Thoracic Surgical Unit, Harefield Hospital, Harefield, Middlesex, United Kingdom

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