Johnjuanb1
01-20-2016, 03:28 AM
I paraphrased this study.
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140 (http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018048/#!po=26.7241)
The stability of RAD140 was high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats (F = 27−63%) and monkeys (65−75%). (This shows high oral bioavailability in primates.)
RAD140 demonstrated excellent affinity for the androgen receptor (Ki = 7 nM vs 29 nM for testosterone and 10 nM for DHT) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor
RAD140 increased the weight of the levator ani muscle above that of the intact control starting with the lowest tested dose (0.1mg/kg). (RAD140 builds muscle at dosing of 10mg in a 220Lb "animal")
Interestingly, RAD140 demonstrated no stimulation of the prostate above the intact animal control level until the highest dose tested, 30 mg/kg.
At 0.3 mg/kg, RAD140 demonstrated muscle efficacy similar to Testosterone Propionate at 0.5 mg/kg. (I interpret this to mean 30mg RAD140 per day builds muscle as effectively as 50mg Testosterone Propionate per day in a 220Lb "animal")
MONKEY DOSING INFO
The results on animal body weight of 28-day dosing with RAD140 at 0.01 mg/kg.
In this study, a mean weight gain of greater than 10% in just 28 days of dosing was achieved at a dose of just 0.1 mg/kg [color="red"]( These monkeys gained 10% muscle in 28 days with the equivalent dose of 10mg per day in a 220Lbs "monkey". That means if you weigh 220Lbs, you would gain 22Lbs of lean muscle in 28 days at 10mg/day, if you respond like a monkey!) [color="red"]
Muscle showed a qualitative trend that increases with dose. Although it appears that the majority of mass increase was due to lean mass increase.
Despite the rather dramatic increases in body weight over such a short time, there was no elevation of liver enzyme transaminase levels in any animal at any dose >2 fold over its baseline value. Given the well-established relationship between oral androgen use and liver stress indicators, we were quite pleased that at a dose 10-fold greater than the fully effective dose we saw minimal liver enzyme elevations.
RAD140 is potency selective, since it stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases. Moreover, it is also efficacy selective, because it is fully anabolic on muscle but demonstrates less than complete efficacy on the prostate and seminal vesicles and, in fact, can partially antagonize the stimulation of the seminal vesicles induced by testosterone. [color="red"](Taking RAD140 simultaneously with testosterone can lower some negative side effects from testosterone)[color="red"]
[b]RAD140 has excellent pharmacokinetics and is a potent anabolic in nonhuman primates as well.
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140 (http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018048/#!po=26.7241)
The stability of RAD140 was high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats (F = 27−63%) and monkeys (65−75%). (This shows high oral bioavailability in primates.)
RAD140 demonstrated excellent affinity for the androgen receptor (Ki = 7 nM vs 29 nM for testosterone and 10 nM for DHT) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor
RAD140 increased the weight of the levator ani muscle above that of the intact control starting with the lowest tested dose (0.1mg/kg). (RAD140 builds muscle at dosing of 10mg in a 220Lb "animal")
Interestingly, RAD140 demonstrated no stimulation of the prostate above the intact animal control level until the highest dose tested, 30 mg/kg.
At 0.3 mg/kg, RAD140 demonstrated muscle efficacy similar to Testosterone Propionate at 0.5 mg/kg. (I interpret this to mean 30mg RAD140 per day builds muscle as effectively as 50mg Testosterone Propionate per day in a 220Lb "animal")
MONKEY DOSING INFO
The results on animal body weight of 28-day dosing with RAD140 at 0.01 mg/kg.
In this study, a mean weight gain of greater than 10% in just 28 days of dosing was achieved at a dose of just 0.1 mg/kg [color="red"]( These monkeys gained 10% muscle in 28 days with the equivalent dose of 10mg per day in a 220Lbs "monkey". That means if you weigh 220Lbs, you would gain 22Lbs of lean muscle in 28 days at 10mg/day, if you respond like a monkey!) [color="red"]
Muscle showed a qualitative trend that increases with dose. Although it appears that the majority of mass increase was due to lean mass increase.
Despite the rather dramatic increases in body weight over such a short time, there was no elevation of liver enzyme transaminase levels in any animal at any dose >2 fold over its baseline value. Given the well-established relationship between oral androgen use and liver stress indicators, we were quite pleased that at a dose 10-fold greater than the fully effective dose we saw minimal liver enzyme elevations.
RAD140 is potency selective, since it stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases. Moreover, it is also efficacy selective, because it is fully anabolic on muscle but demonstrates less than complete efficacy on the prostate and seminal vesicles and, in fact, can partially antagonize the stimulation of the seminal vesicles induced by testosterone. [color="red"](Taking RAD140 simultaneously with testosterone can lower some negative side effects from testosterone)[color="red"]
[b]RAD140 has excellent pharmacokinetics and is a potent anabolic in nonhuman primates as well.