L-Citrulline
Citrulline is a non-essential, non-protein amino acid that forms during the urea cycle and forms ornithine when combined with carbon dioxide. Citrulline is also a critical source of endogenous (natural) arginine, as it is rapidly and efficiently converted to arginine in the vascular endothelium and other tissues.
Citrulline’s benefits have been shown to be greater than its parent compound. While arginine undergoes direct hepatic (liver) metabolism through the enzyme arginase, citrulline bypasses hepatic metabolism entirely and it is delivered straight to the bloodstream. The result is that gut absorption and plasma (blood) bioavailability studies comparing citrulline and arginine have shown two things. First, citrulline is less readily destroyed and has greater absorption than arginine. Second, citrulline supplementation increases arginine levels more effectively than arginine supplementation itself.
This translates to promising results. For example, animal studies show a significant increase in anaerobic performance at a 250mg/kg/day serving of citrulline, while studies in humans implicate citrulline in both aerobic and anaerobic performance increases. As a critical part of the urea cycle, citrulline’s performance benefits are thought to be a result of its role in ammonia clearance. Citrulline is implicated in reducing the oxygen cost of muscle processes, along with increasing the rate of post-exercise ATP and phosphocreatine replenishment. As ATP and phosphocreatine are the body’s ‘exercise fuel,’ this may result in citrulline delaying time to exhaustion in aerobic and anaerobic exercise.
Beta Alanine
Carnosine, a critical compound for muscle function, has long intrigued researchers due to its essential role in buffering pH levels in muscle cells, particularly during intense exercise. However, efforts to increase intramuscular carnosine levels via direct supplementation faced challenges due to rapid degradation in the body. The introduction of beta-alanine, a precursor to carnosine, revolutionized this approach. Beta-alanine has proven to be highly effective in significantly increasing intramuscular carnosine concentrations, thereby unlocking carnosine's beneficial effects on muscle performance. Moreover, beta-alanine itself exhibits physiological benefits beyond its role as a carnosine precursor. By synthesizing carnosine from the precursors L-histidine and l-alanine, carnosine acts as a chemical buffer in muscle cells, crucial for sustained performance during intense exercise. Beta-alanine supplementation has demonstrated consistent and dose-dependent increases in intramuscular carnosine levels, particularly when combined with exercise. This synergy between beta-alanine and exercise promotes not only the direct physiological actions of beta-alanine but also enhances the production of intramuscular carnosine. Consequently, beta-alanine supplementation has been linked to improvements in various aspects of exercise performance, including increased total work capacity, enhanced endurance measured by total time to exhaustion (TTE), and elevated muscle power output. Additionally, beta-alanine supplementation has shown benefits for individuals engaging in power-dependent resistance training and exercising under hypoxic conditions. This comprehensive array of benefits positions beta-alanine as one of the most extensively studied and versatile dietary supplements for enhancing exercise performance and promoting muscle adaptations.
Betaine Anhydrous
Betaine, also known as trimethyl glycine, is a naturally occurring compound found in various living organisms. It serves as a protective agent in non-mammalian animals during osmotic stress and functions as an osmolyte in mammalian tissues, including those of humans. In mammalian cells, betaine is produced through the oxidation of choline and can be acquired from dietary sources such as spinach and beets. Although research on betaine is relatively limited and recent, available literature suggests its potential effects in several areas. Studies investigating betaine supplementation at doses ranging from 1.25g/day to 5g/day for up to 14 days have demonstrated promising results. For instance, one study found that a daily serving of 2.5g enhanced endurance and total repetition volume during exercises like the squat, bench press, and jump squat in healthy, exercise-trained adults. Another study reported increased peak power, maximum peak power, force, and the maintenance of force and power in similar subjects with the same dosage of betaine. Moreover, research exploring betaine's impact on the endocrine system has shown potential effects on various endocrine processes. These findings have led researchers to hypothesize that longer-term betaine supplementation may enhance the hypertrophic response to resistance training, indicating its potential as a performance-enhancing supplement in the realm of exercise physiology.
L-Tyrosine
Tyrosine is amongst a class of amino acids known as ‘non-essential’ amino acids, so called because the body can produce them endogenously, and it is therefore not essential to consume dietary tyrosine. That said, tyrosine is also what is known as a conditionally essential amino acid; conditionally essential because, along with glucose and ammonia, the synthesis of tyrosine additionally requires adequate levels of phenylalanine. Once synthesized, tyrosine is one of the most critical amino acids, given its prominent role as a substrate in the synthesis of the catecholamines dopamine, norepinephrine, and epinephrine, in addition to both T3 (triiodothyronine) and T4 (thyroxine) thyroid hormones.
In studies on stress modulation, tyrosine has been demonstrated to reverse stress-induced norepinephrine depletion and the depressant-behavioral effects normally associated with it. In simpler terms, tyrosine may, in certain conditions, dampen the extent to which norepinephrine is removed from the bloodstream during a stress event. In simpler terms still, tyrosine may help to mitigate the sense of depletion and fatigue felt at the end of a workout.
Tyrosine may also play important metabolic functions, mostly related to its role in synthesizing compounds which stimulate the nervous system. While not traditionally considered a sympathomimetic amine, studies which have coadministered tyrosine and stimulants demonstrate a synergistic effect. These studies suggest that tyrosine may potentiate the effects of both endogenous and supplemental norepinephrine and its mimetics (in the case of exogenous use) with respect to lipolysis, thermogenesis, and energy expenditure. Meaning that tyrosine may play a role in assisting norepinephrine to break up triglycerides and increase body heat transiently.
Alpha-GPC 50% (L-Alpha-Glycerylphosphorylcholine)
Among the various choline pro-drugs or precursors, Alpha GPC stands out for its significant impact on circulating choline levels. Choline, an essential nutrient, plays a crucial role in numerous metabolic pathways, including DNA regulation, protein function, and metabolism. Notably, choline serves as a precursor for the synthesis of acetylcholine, a critical neurotransmitter involved in various physiological functions, such as muscular contraction and cognitive processes like memory and learning. Animal studies have underscored the importance of choline in prenatal brain development, with maternal choline levels directly influencing offspring brain development, particularly in the hippocampus, a region vital for memory consolidation and learning in humans. Given choline's role as a substrate for acetylcholine synthesis, it may indirectly impact these cognitive processes. Recent research involving Alpha GPC supplementation has shown promising results in enhancing power output. In a placebo-controlled, double-blind, randomized trial involving healthy volunteers, those supplemented with Alpha GPC experienced a significant 14% increase in bench press performance compared to the placebo group. Researchers attribute this improvement to Alpha GPC's potential to acutely elevate growth hormone levels, highlighting its potential as an ergogenic aid in enhancing physical performance.
Caffeine Anhydrous
Caffeine is one of the most widely consumed, and perhaps one of the most reviewed, psychoactive compounds. Its physiological effects in a range of areas have been well-documented, including exercise performance, information processing, alertness and mood enhancement, attention, and awareness, along with its anti-lipogenic and lipolytic abilities.
Most importantly to FBOMB, caffeine has been shown to have significant effects on exercise performance, even with ingestion in servings as small 3 to 9mg/kg/bw/day (the equivalent of 2 cups of standard coffee, for a 170lb male). In endurance training, possible explanations for caffeine’s performance-enhancing effects lie in its metabolic effects on both lean and fat tissue. It is suggested that caffeine’s potent lipolytic (the breakdown of fat tissue into fatty acids) and oxidative (the actual ‘burning’ of fat) action allow the body to utilize these sources during prolonged submaximal exercise. Consequently, muscle glycogen is spared and available for use later in the training session. Practically speaking, this means caffeine is forcing your body to preferentially use fat tissue as a fuel source, while sparing the glycogen which gives you the full-bodied look!
In short-term exercise, caffeine’s demonstrated role in the inhibition of cyclic AMP- phosphodiesterase’s (PDE), adenosine receptor antagonism, and adrenoreceptor agonism come into play. These three pathways collectively stimulate lipolytic activity, boost fat metabolism, increase metabolic rate and energy expenditure, and regulate the body’s thermogenic activity. The practical results of activating these pathways are increases to the contractile force of both cardiac and skeletal muscle (harder flexion), an increase in energy expenditure (freeing up more caloric energy to be used in contraction), dilation of vasculature (better blood flow), and improvements to both nitrogen retention and skeletal muscle protein synthesis (key components to muscle building).
Vasodrive-AP® (Isoleucyl-prolyl-proline (IPP) and Valyl-prolyl-proline (VPP) (from hydrolyzed milk casein)
Vasodrive-AP® is a patented dietary supplement ingredient composed of a precise blend of naturally derived peptides, primarily derived from casein hydrolysate. This ingredient has garnered attention for its potential benefits in enhancing exercise performance through its vasodilatory properties. Vasodrive-AP® works by promoting the release of nitric oxide (NO), a key signaling molecule involved in vasodilation, which leads to the relaxation of blood vessels and increased blood flow to exercising muscles. It does this through several mechanisms of action. First, the increase in the production of endothelial nitric oxide synthase (eNOS) improve arterial flexibility leading to enhanced blood flow. Second, Vasodrive-AP® can also inhibit the enzyme that leads to the constriction of blood vessels. By improving blood flow and oxygen delivery to working muscles, Vasodrive-AP® may enhance exercise capacity, delay the onset of fatigue, and improve overall performance during both endurance and resistance training activities. Additionally, the improved nutrient and oxygen delivery facilitated by Vasodrive-AP® may aid in muscle recovery post-exercise, potentially reducing muscle soreness and accelerating the repair process. While further research is needed to fully elucidate its mechanisms and optimal dosages, Vasodrive-AP® shows promise as a natural ergogenic aid for individuals seeking to maximize their exercise performance and recovery.
Pine Bark Extract (Pinus pinaster)(std. 95% proanthocyanidins)
Pine bark extract can have an impact on nitric oxide (NO) levels in the body, which are responsible for vasodilation and improving blood flow. It can also control oxidative stress by scavenging reactive oxygen and nitrogen species and suppressing production of peroxides thus improving recovery rates. Pine bark contains bioflavonoids that act as antioxidants, which help protect the body from oxygen waste and other biproducts that can cause cell damage. A 2020 study examined the impact of pine bark extract on exercise performance and recovery in test subjects over the span of 14 days. Metrics included presence of muscle damage, oxidative stress, and inflammation. Results in the 20 test subjects revealed that pine bark extract may help protect the muscle from negative effects of free radicals. With the dual benefits of increased nitric oxide and improvements in recovery muscle health, pine bark extract can be a useful addition to any pre-workout formula, which is why we included it in this product.
Dicaffeine Malate
Dicaffeine malate, by definition, is two caffeine molecules bonded to a malic acid molecule. What this unique combination does is offer some distinct advantages when combined with caffeine anhydrous, as well as in combination with traditional caffeine. We all know that the benefits of caffeine can include increased energy, enhanced focus and cognitive performance, boosts in metabolism, improved reaction time, etc. What is less known are the benefits of malic acid. Malic acid can promote energy production through the Krebs cycle, increase endurance, enhance power output, and help delay muscle fatigue. So, separating these two ingredients offer some wide benefits, but together they can complement each other a great deal. What dicaffeine malate can offer for an individual is a slow released caffeine source that can eliminate normal jitters, anxiousness, and no crash. This also can lead to a longer lasting caffeine, usually around 6-8 hours, so you’ll be able to get through your grueling training sessions as well as feel energized post training. Dicaffeine malate can also offer energy replenishment through malic acids role in the breakdown of carbs, fats, and proteins and it can also help reduce caffeine tolerance.
So, caffeine on its own can have a host of benefits from an efficiency standpoint as being a tried-and-true ergogenic aid but with normal caffeine having a relatively fast half-life, we can reap extra benefits from a more delayed release caffeine to our pre-workout formulas. It is to be noted that because of the combination of caffeine and malic acid, the % breakdown is 75% caffeine and 25% malic acid. So, the 150mg of dicaffeine malate in this product yields 112.5mg of active caffeine. With the 300mg of caffeine anhydrous listed above, as well as the 100mg of caffeine citrate below (yielding 50mg caffeine) we have a whopping 462.5mg of active caffeine in this explosive pre-workout!
Skullcap Powder (Scutellaria baicalensis) (whole herb)
Skullcap powder, derived from the aerial parts of the Scutellaria genus, presents potential benefits for exercise performance and recovery. Rich in bioactive compounds like flavonoids and polyphenols, skullcap powder exhibits anti-inflammatory and antioxidant properties that may support exercise-related outcomes. Studies suggest that skullcap supplementation could mitigate exercise-induced inflammation and oxidative stress, thereby aiding in muscle recovery and reducing post-exercise soreness. Additionally, skullcap's potential anxiolytic and stress-reducing effects may promote mental resilience during intense training periods, potentially enhancing focus and motivation. While further research is needed to elucidate the specific mechanisms and optimal dosages for exercise benefits, skullcap powder holds promise as a natural adjunct to exercise regimes, particularly for individuals seeking to optimize recovery and performance.
Caffeine Citrate
Caffeine citrate is not generally seen in the typical sports performance area. It is more commonly prescribed for premature infants for a short time for the treatment of apnea of prematurity. Apnea of prematurity occurs when a premature infant does not breathe for 15-20 seconds during sleep. In addition to this caffeine citrate can at times be prescribed for migraines in some individuals.
Recently caffeine citrate has gained some popularity in sports performance as it appears to be able to raise blood caffeine levels faster than other caffeine sources. This allows for a quicker feeling of increased energy. For example, typical caffeine levels peak at about 60-120 minutes post ingestion of caffeine anhydrous, whereas blood levels peak around 30 minutes post-ingestion for caffeine citrate. The one drawback to caffeine citrate is that it provides 50% less caffeine per dose than caffeine anhydrous. The specific blend of caffeine sources we have used in Castle Bravo complement each other through differing release times, meaning you will have a quick and effective stimulant feeling with caffeine citrate, as well as plenty of caffeine anhydrous, to give you the quick hitting and long-lasting energy you need to get through your workouts.
Bitter Orange Extract (Citrus aurantium) (std. 30% synephrine)
Bitter orange extract, derived from the fruit of Citrus aurantium, contains a diverse array of bioactive compounds, notably including synephrine, flavonoids, and essential oils. Synephrine, the principal alkaloid in bitter orange extract, exhibits sympathomimetic properties, stimulating the sympathetic nervous system and potentially increasing heart rate, blood pressure, and metabolic rate. These effects have led to interest in bitter orange extract as a potential aid for weight management, with studies suggesting its ability to enhance thermogenesis, suppress appetite, and stimulate lipolysis. The flavonoids present in bitter orange extract contribute antioxidant activity, which may offer additional health benefits by protecting cells from oxidative damage. Additionally, the combination of caffeine and synephrine appears to potentiate each ingredient’s effects – with rates of fatty acid liberation, heart rate, metabolic rate, and fatty acid oxidation increased in clinical trials featuring the combination. In several studies utilizing other forms of synephrine, it was found that the combination of synephrine and caffeine led to a small but significant reduction in fat mass of 3lbs, and a reduction in bodyfat of 2.9%.
Astragin® (Astragalus membranaceous and Panax notoginseng Root Extracts)
AstraGin® is a trademarked combination of Astragalus membranaceous and Panax notoginseng that has been widely used in the supplement manufacturing industry largely for due to its clinically studied benefits for improving absorption of nutrients, peptides, and amino acids. Some statistics include increased absorption of creatine, leucine, citrulline, and other peptides by up to 67%, increased curcumin absorption by 92%, increases polyunsaturated fatty acids (from flax and fish oil) by 58% and 100% respectively, as well as can increase ATP production in the liver by 18%. AstraGin® has been shown capable of increasing muscle protein synthesis and increased mTOR through enhanced leucine absorption, which has an influence on improved glucose metabolism and mitochondrial functions. In addition to this benefit, AstraGin’s® ability to enhance polyunsaturated fatty acid absorption while also inhibiting saturated fatty acid absorption, thus reducing the risk of impaired glucose metabolism and mitochondrial function, can enhance ATP synthesis through mitochondrial respiration, and increase oxidative phosphorylation.
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