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Today in physiology we where reading on adrenergic receptors in the body and the β3 is most intriguing. As of 2 minutes of research I found an article that might intrigue some of you so I decided to share.
Actions of the β3 receptor include:
Enhancement of lipolysis in adipose tissue.[2]
Thermogenesis in skeletal muscle[3]
It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β3 agonists have demonstrated antistress effects in animal studies, suggesting it also has a role in the CNS. Beta3-Receptors are found in the gallbladder, urinary bladder, and in brown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination.
Clinical Pharmacology & Therapeutics - Abstract of article: Acute effect of L-796568, a novel [beta]3-adrenergic receptor agonist, on energy expenditure in obesemen[ast]
Abstract
Objective: Our objective was to investigate the thermogenic efficacy of single oral doses of the novel beta3-adrenergic receptor agonist L-796568 [(R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]-phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]-benzenesulfonamide, dihydrochloride] inhumans.
Methods: Twelve healthy overweight to obese men participated in this 2-center, 3-period, randomized, placebo-controlled, crossover trial. In each period subjects received 250 mg L-796568, 1000 mg L-796568, or placebo. Energy expenditure and respiratory quotient were determined by indirect calorimetry; blood samples were taken; and ear temperature, heart rate, and blood pressure were measured at baseline and during the 4-hour period after administration.
Results: Energy expenditure increased significantly after the 1000-mg dose (about 8%) and this was accompanied by an increase in plasma glycerol and free fatty acid concentrations. Systolic blood pressure also increased significantly. No changes in heart rate, diastolic blood pressure, ear temperature, plasma catecholamine, potassium, orleptin were found.
Conclusions: Single-dose administration of 1000 mg of the novel beta3-adrenergic receptor agonist L-796568 increased lipolysis and energy expenditure in overweight men. This is the first study to show such an effect of beta3-adrenergic receptor agonists in humans without significant evidence for beta2-adrenergic receptor involvement.
If some of these compounds work without being agonists of β1 and β2 receptors these could easily be safe alternatives to clen and be much more effective.
Actions of the β3 receptor include:
Enhancement of lipolysis in adipose tissue.[2]
Thermogenesis in skeletal muscle[3]
It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β3 agonists have demonstrated antistress effects in animal studies, suggesting it also has a role in the CNS. Beta3-Receptors are found in the gallbladder, urinary bladder, and in brown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination.
Clinical Pharmacology & Therapeutics - Abstract of article: Acute effect of L-796568, a novel [beta]3-adrenergic receptor agonist, on energy expenditure in obesemen[ast]
Abstract
Objective: Our objective was to investigate the thermogenic efficacy of single oral doses of the novel beta3-adrenergic receptor agonist L-796568 [(R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]-phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]-benzenesulfonamide, dihydrochloride] inhumans.
Methods: Twelve healthy overweight to obese men participated in this 2-center, 3-period, randomized, placebo-controlled, crossover trial. In each period subjects received 250 mg L-796568, 1000 mg L-796568, or placebo. Energy expenditure and respiratory quotient were determined by indirect calorimetry; blood samples were taken; and ear temperature, heart rate, and blood pressure were measured at baseline and during the 4-hour period after administration.
Results: Energy expenditure increased significantly after the 1000-mg dose (about 8%) and this was accompanied by an increase in plasma glycerol and free fatty acid concentrations. Systolic blood pressure also increased significantly. No changes in heart rate, diastolic blood pressure, ear temperature, plasma catecholamine, potassium, orleptin were found.
Conclusions: Single-dose administration of 1000 mg of the novel beta3-adrenergic receptor agonist L-796568 increased lipolysis and energy expenditure in overweight men. This is the first study to show such an effect of beta3-adrenergic receptor agonists in humans without significant evidence for beta2-adrenergic receptor involvement.
If some of these compounds work without being agonists of β1 and β2 receptors these could easily be safe alternatives to clen and be much more effective.
