Potential anti-diabetic applications of a new molecule with affinity for β3-Adrenoceptors

Barrionuevo, M; Milagro, Fermı́n I.; Cenarruzabeitia, Edurne; Ja, Martínez

doi:10.1016/0024-3205(96)00395-5

Cited by 16 publications

(13 citation statements)

References 12 publications

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“…Trecadrine administration decreased plasma insulin concentrations in control and diet induced obese animals, which may be associated with the reduction in visceral fat and insulin resistance as well as a higher glucose utilization by tissues, as previously reported, 15 since plasma glucose and insulin concentrations followed a parallel trend.…”

Section: Discussionsupporting

confidence: 82%

“…24 ± 26 Thus, b 3 -adrenoceptors are expressed in WAT, BAT, skeletal muscle, heart, brain, airway tissues and gastrointestinal tissues of rodents, while in humans the b 3 -adrenoceptor mRNA has been reported to occur at least in WAT, BAT, gallbladder and colon. 4 In this context, Trecadrine, a molecule with high af®nity for b 3 -adrenoceptors and with anti-diabetic properties, 15 has been tested for its effectiveness and mechanistic involvement in a dietary obesity model. Rats eating a cafeteria diet for 75 days increased body weight, total fat content and BAT and WAT weights.…”

Section: Discussionmentioning

confidence: 99%

“…Trecadrine, a diphenyl-methylene-ethylamine derivative compound, whose formula and characterization as a b 3 -adrenergic agonist agent have been previously published, 15 was supplied by Wassermann-Chiesi (BarcelonaaMilano).…”

Section: Drugmentioning

confidence: 99%

“…In the current study, the aims were to assess the impact of a recently developed b 3 -adrenergic agonist, Trecadrine, 7,8,15 on body composition, plasma insulin and leptin as well as on the mRNA expression levels of several genes involved in body weight homeostasis and thermoregulation (OB, UCP1 and UCP2 in WAT, BAT and gastrocnemius muscle, respectively) in lean and obese animals, which were fed a cafeteria diet.…”

Section: Introductionmentioning

confidence: 99%

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Up-regulation of muscle UCP2 gene expression by a new β3-adrenoceptor agonist, trecadrine, in obese (cafeteria) rodents, but down-regulation in lean animals

Berraondo

Marti

Duncan³

et al. 2000

Int J Obes

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OBJECTIVE: The anti-obesity properties of a new b 3 -adrenergic agonist (Trecadrine) were examined in a diet-induced obesity model, including the effects on OB and uncoupling protein (UCP-1 and -2) gene expression. MEASUREMENTS: Control rats and cafeteria-fed rats were treated with placebo or Trecadrine for 35 days. Leptin and UCP (1 and 2) mRNA levels were determined by reverse transcription ± polymerase chain reaction (RT-PCR) methodology in adipose tissue and gastrocnemius muscle. RESULTS: Animals fed a cafeteria diet increased body weight, fat content, white adipose tissue (WAT), brown adipose tissue (BAT) weights and oxygen consumption in relation to lean controls. A rise in plasma leptin, WAT OB gene expression as well as circulating free fatty acids levels was found in obese rats as compared with lean controls. Trecadrine administration to cafeteria-fed animals decreased fat content, WAT weight, circulating leptin and fatty acids concentrations, and WAT OB gene expression, reaching comparable values to lean controls, while WAT O 2 consumption was increased in these animals. Also, an increase in BAT UCP1 mRNA levels was found through a twoway analysis of variance in control and obese animals after Trecadrine administration. Gastrocnemius muscle UCP2 gene expression was reduced in lean Trecadrine-treated and diet-induced obese animals as compared to controls, while an increase was found in cafeteria-fed animals after Trecadrine administration. A negative correlation between WAT O 2 consumption and UCP2 expression was found in control animals, but not in the cafeteria-fed groups, suggesting a differential response to the b 3 -adrenergic compound in lean and obese animals, which is in agreement with the reported statistical interactions between obesity and Trecadrine administration found for WAT O 2 consumption and muscle UCP2 expression, as well as for plasma leptin and WAT leptin expression. CONCLUSION: The new b 3 -adrenergic agonist, Trecadrine, decreases fat content and increases gastrocnemius muscle UCP2 gene expression in a diet-induced obesity model. This sheds additional light on the action mechanism of compounds with af®nity for b 3 -adrenoceptors and other potential anti-obesity agents.

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Section: Discussionsupporting

confidence: 82%

Section: Discussionmentioning

confidence: 99%

Section: Drugmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Up-regulation of muscle UCP2 gene expression by a new β3-adrenoceptor agonist, trecadrine, in obese (cafeteria) rodents, but down-regulation in lean animals

Berraondo

Marti

Duncan³

et al. 2000

Int J Obes

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“…Rectal temperature of the rats was measured prior to i.p. injections of: saline, leptin (Peprotech, London, UK; 0.25 mg/kg) or the b 3 -AR agonist Trecadrine (Wasserman-Chiesi, Barcelona/Milan; 1 mg/kg, see reference (Barrionuevo et al, 1996) for chemical structure and pharmacological properties). The doses tested were used based on previous experiments showing physiological effects (Pelleymounter et al, 1995;Gó mez-Ambrosi et al, 1999).…”

Section: Animals and Proceduresmentioning

confidence: 99%

Rapid in vivo PGC-1 mRNA upregulation in brown adipose tissue of Wistar rats by a β3-adrenergic agonist and lack of effect of leptin

Gómez-Ambrosi

Frühbeck

Martínéz

2001

Molecular and Cellular Endocrinology

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Peroxisome proliferator-activated receptor-g coactivator-1 (PGC-1) is highly expressed in brown adipose tissue (BAT) and plays an important role in adaptive thermogenesis. The aim of this study was to assess the acute effect of a b 3 -adrenergic agonist (Trecadrine) and leptin on the expression of PGC-1 and PPARg2 mRNA in BAT. Trecadrine produced a marked increase (4.5-fold) in PGC-1 mRNA compared to controls (PB0.001) without changes in PPARg2 mRNA, whereas leptin administration did not alter either PGC-1 or PPARg2 expression. These results show that selective stimulation of the b 3 -adrenoceptor rapidly upregulates the expression of PGC-1 in brown adipocytes without a concomitant increase in PPARg2. Moreover, our results show that PGC-1 and PPARg2 expression in BAT seems not to be acutely regulated by leptin.

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Effects of a β3-Adrenergic Agonist on Glucose Uptake and Leptin Expression and Secretion in Cultured Adipocytes from Lean and Overweight (Cafeteria) Rats

Moreno-Aliaga

Lamas

Marti

et al. 2002

Biochemical and Biophysical Research Communications

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Potential anti-diabetic applications of a new molecule with affinity for β3-Adrenoceptors

Cited by 16 publications

References 12 publications

Up-regulation of muscle UCP2 gene expression by a new β3-adrenoceptor agonist, trecadrine, in obese (cafeteria) rodents, but down-regulation in lean animals

Up-regulation of muscle UCP2 gene expression by a new β3-adrenoceptor agonist, trecadrine, in obese (cafeteria) rodents, but down-regulation in lean animals

Rapid in vivo PGC-1 mRNA upregulation in brown adipose tissue of Wistar rats by a β3-adrenergic agonist and lack of effect of leptin

Effects of a β3-Adrenergic Agonist on Glucose Uptake and Leptin Expression and Secretion in Cultured Adipocytes from Lean and Overweight (Cafeteria) Rats

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