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Beta-3 adenergic receptors are primarily located on adipose tissue cells. Direct stimulation of these receptors is believed to cause lipolysis. Here is some info I have:
Piperidine, pyrrolidine, and azetidine sulfonamides were examined as linkers in designing novel human beta(3) adrenergic receptor (beta(3)-AR) agonists. The azetidine derivative 37, and piperidine derivatives 7, 8, and 13 were found to be potent beta(3)-AR agonists and have good selectivity against beta(1)- and beta(2)-AR.
THIS IS GOOD NEWS. YOU WANT THE FAT BURNING EFFECTS WITHOUT THE CARDIO SIDES.
Acute effect of L-796568, a novel beta 3-adrenergic receptor agonist, on energy expenditure in obese men.
Clin Pharmacol Ther 2002 Apr;71(4):272-9 (ISSN: 0009-9236)
van Baak MA; Hul GB; Toubro S; Astrup A; Gottesdiener KM; De Smet M; Saris WH
Nutrition and Toxicology Research Institute (NUTRIM), Department of Human Biology, Maastricht University, The Netherlands. [email protected].
OBJECTIVE: Our objective was to investigate the thermogenic efficacy of single oral doses of the novel beta(3)-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] in humans. 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, or leptin were found. CONCLUSIONS: Single-dose administration of 1000 mg of the novel beta(3)-adrenergic receptor agonist L-796568 increased lipolysis and energy expenditure in overweight men. This is the first study to show such an effect of beta(3)-adrenergic receptor agonists in humans without significant evidence for beta(2)-adrenergic receptor involvement.
From METABOLIC PHARMACEUTICALS LIMITED (AUSTRALIA):
Basis for the Technology
Growth hormone occurs naturally in the body and, as its name suggests, causes growth. When administered to humans, growth hormone also causes body fat reduction. This occurs by lipolysis (breakdown of fat into basic chemical components), anti lipogenesis (reduction of the rate of synthesis of fat from its chemical components), and an increase in resting energy expenditure.
However, because growth hormone affects more than just fat metabolism, it cannot be used as an effective anti obesity drug. One major undesirable effect of treatment with growth hormone is resistance to the actions of insulin which may lead to diabetes, at best limiting the dose which may be given. Other unwanted effects are associated with muscle and organ growth which cannot be sustained with long term treatment.
Associate Professor Ng at Monash University and his co-workers have established that there is a small region of the growth hormone molecule, less than one tenth of its total size, denoted hGH 177-191, which appears to be responsible for its specific effect on fat and appears not to have any effect on growth or on insulin resistance.
AOD9604 is a peptide variant of hGH 177-191.
Comparative Advantages
Metabolic believes that AOD has two important features which enhance its chance of success:
• AOD acts directly on the metabolism of fat. The Directors believe that a treatment which is not dependent on behavioural modification such as appetite suppression and its associated side effects has an enhanced chance of acceptance by both patient and doctor.
• The structural design of AOD is based on human growth hormone and the rationale for its design is the known effect of growth hormone on body fat in humans. Because of this link, extrapolations of laboratory results from rodents and pigs to humans are viewed by the Directors as having a comparatively strong basis. As the rate of fat loss observed in short term trials of growth hormone in obese people is about 0.5 kg per week compared to placebo, the same is predicted for AOD9604. If maintained in long term dosing over several months, AOD9604 will be at least twice as effective as current drugs.
NOT DIRECTLY ON-TOPIC, BUT MANY STILL BELIEVE THAT HGH HAS SOME EFFECT VIA BETA-3 ADENERGIC RECEPTORS.
Piperidine, pyrrolidine, and azetidine sulfonamides were examined as linkers in designing novel human beta(3) adrenergic receptor (beta(3)-AR) agonists. The azetidine derivative 37, and piperidine derivatives 7, 8, and 13 were found to be potent beta(3)-AR agonists and have good selectivity against beta(1)- and beta(2)-AR.
THIS IS GOOD NEWS. YOU WANT THE FAT BURNING EFFECTS WITHOUT THE CARDIO SIDES.
Acute effect of L-796568, a novel beta 3-adrenergic receptor agonist, on energy expenditure in obese men.
Clin Pharmacol Ther 2002 Apr;71(4):272-9 (ISSN: 0009-9236)
van Baak MA; Hul GB; Toubro S; Astrup A; Gottesdiener KM; De Smet M; Saris WH
Nutrition and Toxicology Research Institute (NUTRIM), Department of Human Biology, Maastricht University, The Netherlands. [email protected].
OBJECTIVE: Our objective was to investigate the thermogenic efficacy of single oral doses of the novel beta(3)-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] in humans. 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, or leptin were found. CONCLUSIONS: Single-dose administration of 1000 mg of the novel beta(3)-adrenergic receptor agonist L-796568 increased lipolysis and energy expenditure in overweight men. This is the first study to show such an effect of beta(3)-adrenergic receptor agonists in humans without significant evidence for beta(2)-adrenergic receptor involvement.
From METABOLIC PHARMACEUTICALS LIMITED (AUSTRALIA):
Basis for the Technology
Growth hormone occurs naturally in the body and, as its name suggests, causes growth. When administered to humans, growth hormone also causes body fat reduction. This occurs by lipolysis (breakdown of fat into basic chemical components), anti lipogenesis (reduction of the rate of synthesis of fat from its chemical components), and an increase in resting energy expenditure.
However, because growth hormone affects more than just fat metabolism, it cannot be used as an effective anti obesity drug. One major undesirable effect of treatment with growth hormone is resistance to the actions of insulin which may lead to diabetes, at best limiting the dose which may be given. Other unwanted effects are associated with muscle and organ growth which cannot be sustained with long term treatment.
Associate Professor Ng at Monash University and his co-workers have established that there is a small region of the growth hormone molecule, less than one tenth of its total size, denoted hGH 177-191, which appears to be responsible for its specific effect on fat and appears not to have any effect on growth or on insulin resistance.
AOD9604 is a peptide variant of hGH 177-191.
Comparative Advantages
Metabolic believes that AOD has two important features which enhance its chance of success:
• AOD acts directly on the metabolism of fat. The Directors believe that a treatment which is not dependent on behavioural modification such as appetite suppression and its associated side effects has an enhanced chance of acceptance by both patient and doctor.
• The structural design of AOD is based on human growth hormone and the rationale for its design is the known effect of growth hormone on body fat in humans. Because of this link, extrapolations of laboratory results from rodents and pigs to humans are viewed by the Directors as having a comparatively strong basis. As the rate of fat loss observed in short term trials of growth hormone in obese people is about 0.5 kg per week compared to placebo, the same is predicted for AOD9604. If maintained in long term dosing over several months, AOD9604 will be at least twice as effective as current drugs.
NOT DIRECTLY ON-TOPIC, BUT MANY STILL BELIEVE THAT HGH HAS SOME EFFECT VIA BETA-3 ADENERGIC RECEPTORS.
