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kallmekrash
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For the less technically inclined:
http://www.nytimes.com/aponline/health/AP-Weight-Loss-Thyroid.html
Technical description of KB141 compared to T3 below:
Pharmacologic profile of thyroid hormone-beta agonists: Differential effects on metabolic rate, cardiac function and cholesterol
Gary Grover, Ph.D., Sr. Principal Scientist, Bristol-Myers Squibb Company, Lawrenceville, NJ
Thyroid hormone regulates metabolic rate in vivo by affecting lipid metabolism, energy substrate utilization and a number of other activities. The effects of thyroid hormone are mediated by thyroid receptor subtypes (TR). TR¥á1 is expressed ubiquitously while TR©¬ is found primarily in liver, pituitary and the CNS. TR¥á1-/- mice have lower basal heart rate (HR) and lower body temperature but a normal cholesterol response to T3. TR©¬-/- mice have a normal HR. To determine the role of TR©¬ in the regulation of metabolic rate (MR), TR¥á1-/- mice were used to examine the effects of T3 mediated by TR©¬ (primarily). These studies were a collaboration between Bristol-Myers Squibb and Karo-Bio. KB141 is an analogue of T3 with chloride instead of iodine. KB141 is 13-15-fold more selective for TR©¬ vs TR¥á1 and is a full agonist at TR©¬. KB141 is 27-fold more selective for cholesterol lowering effects vs. HR and 9-fold more selective for effects on MR vs. HR. The positive control, T3, caused cardiac hypertrophy due to volume overload while KB141 had no effect on cardiac mass at doses up to 1000 mg/kg/d. In normal, lean cynomologous monkeys, KB141 lowered cholesterol by 30% at the high dose after 30 days with no effect on HR. Scientists were unable to identify a dose of T3 that would lower cholesterol without affecting HR. There was a dose dependent decrease in body weight that was due primarily to loss of adipose tissue mass. Similar changes were observed in obese monkeys. Both TR¥á and TR©¬ agonists can mediate an increase in metabolic rate. However, TR©¬ agonists exhibit a decreased slope for the potency curve allowing the effects on MR to be separated from effects on HR. Therefore, a TR©¬ selective agonist should be an effective anti-obesity drug by increasing metabolic rate without producing adverse effects on the cardiovascular system.
http://www.nytimes.com/aponline/health/AP-Weight-Loss-Thyroid.html
Technical description of KB141 compared to T3 below:
Pharmacologic profile of thyroid hormone-beta agonists: Differential effects on metabolic rate, cardiac function and cholesterol
Gary Grover, Ph.D., Sr. Principal Scientist, Bristol-Myers Squibb Company, Lawrenceville, NJ
Thyroid hormone regulates metabolic rate in vivo by affecting lipid metabolism, energy substrate utilization and a number of other activities. The effects of thyroid hormone are mediated by thyroid receptor subtypes (TR). TR¥á1 is expressed ubiquitously while TR©¬ is found primarily in liver, pituitary and the CNS. TR¥á1-/- mice have lower basal heart rate (HR) and lower body temperature but a normal cholesterol response to T3. TR©¬-/- mice have a normal HR. To determine the role of TR©¬ in the regulation of metabolic rate (MR), TR¥á1-/- mice were used to examine the effects of T3 mediated by TR©¬ (primarily). These studies were a collaboration between Bristol-Myers Squibb and Karo-Bio. KB141 is an analogue of T3 with chloride instead of iodine. KB141 is 13-15-fold more selective for TR©¬ vs TR¥á1 and is a full agonist at TR©¬. KB141 is 27-fold more selective for cholesterol lowering effects vs. HR and 9-fold more selective for effects on MR vs. HR. The positive control, T3, caused cardiac hypertrophy due to volume overload while KB141 had no effect on cardiac mass at doses up to 1000 mg/kg/d. In normal, lean cynomologous monkeys, KB141 lowered cholesterol by 30% at the high dose after 30 days with no effect on HR. Scientists were unable to identify a dose of T3 that would lower cholesterol without affecting HR. There was a dose dependent decrease in body weight that was due primarily to loss of adipose tissue mass. Similar changes were observed in obese monkeys. Both TR¥á and TR©¬ agonists can mediate an increase in metabolic rate. However, TR©¬ agonists exhibit a decreased slope for the potency curve allowing the effects on MR to be separated from effects on HR. Therefore, a TR©¬ selective agonist should be an effective anti-obesity drug by increasing metabolic rate without producing adverse effects on the cardiovascular system.
