Pharmacology of Moxonidine, an I1-Imidazoline Receptor Agonist

Ziegler, Dieter; Haxhiu, Musa A.; Kaan, E. C.; Papp, Julius Gy.; Ernsberger, Paul

doi:10.1097/00005344-199627003-00005

Cited by 62 publications

(41 citation statements)

References 120 publications

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“…Moreover, it improves glucose tolerance and decreases plasma insulin levels in these animals and in fructose-fed rats (Ernsberger et al, 1996;Rosen et al, 1997) and obese hypertensive patients (Lithell, 1997), implying that moxonidine may improve insulin sensitivity. Moxonidine is thought to act primarily as a selective agonist at imidazoline I 1 receptors (Ziegler et al, 1996) that are mainly located in the rostro-ventrolateral medulla of the brain stem, and also in the hypothalamus (Kaan et al, 1995;Olmos et al, 1992;GarciaSevilla, 1997). The role of imidazoline I 1 receptors in the central control of appetite and body weight is uncertain, as are the neuronal pathways and neurotransmitters that moxonidine might in¯uence to reduce feeding.…”

Section: Introductionmentioning

confidence: 99%

The effect of moxonidine on feeding and body fat in obese Zucker rats: role of hypothalamic NPY neurones

Chen

King

Pickavance

et al. 1999

British J Pharmacology

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1 The antihypertensive agent moxonidine, an imidazoline I i -receptor agonist, also induces hypophagia and lowers body weight in the obese spontaneously hypertensive rat, but the central mediation of this action and the neuronal pathways that moxonidine may interact with are not known. We studied whether moxonidine has anti-obesity e ects in the genetically-obese and insulinresistant fa/fa Zucker rat, and whether these are mediated through inhibition of the hypothalamic neuropeptide Y (NPY) neurones. 2 Lean and obese Zucker rats were given moxonidine (3 mg kg 71 day 71 ) or saline by gavage for 21 days. 3 Moxonidine decreased food intake throughout by 20% in obese rats (P50.001) and by 8% in lean rats (P50.001), and reduced weight gain that ®nal body weight was 15% lower in obese (P50.001) and 7% lower in lean (P50.01) rats than their untreated controls. Plasma insulin and leptin levels were decreased in moxonidine-treated obese rats (P50.01 and P50.05), but unchanged in treated lean rats. Uncoupling protein-1 gene expression in brown adipose tissue was stimulated by 40 ± 50% (P40.05) in both obese and lean animals given moxonidine. Obese animals given moxonidine showed a 37% reduction in hypothalamic NPY mRNA levels (P=0.01), together with signi®cantly increased NPY concentrations in the paraventricular nucleus (P50.05), but no changes in the arcuate nucleus or other nuclei; this is consistent with reduced NPY synthesis in the arcuate nucleus and blocked release of NPY in the paraventricular nucleus. In lean animals, moxonidine did not a ect NPY levels or NPY mRNA. 4 The hypophagic, thermogenic and anti-obesity e ects of moxonidine in obese Zucker rats may be partly due to inhibition of the NPY neurones, whose inappropriate overactivity may underlie obesity in this model.

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Section: Introductionmentioning

confidence: 99%

The effect of moxonidine on feeding and body fat in obese Zucker rats: role of hypothalamic NPY neurones

Chen

King

Pickavance

et al. 1999

British J Pharmacology

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“…Besides this direct effect on sympathetic tone, in contrast to beta-blockers, moxonidine induces vasodilatation with no change in cardiac output and little change in heart rate and it increases insulin sensitivity in insulin-resistant subjects. 8,9 Our pilot study shows that centrally acting sympatholytic agent (moxonidine) may have a positive effect on erectile function. It also seemed to increase penile circulation compared to the effect of a beta-blocker (metoprolol).…”

Section: Discussionmentioning

confidence: 88%

Effects of moxonidine and metoprolol in penile circulation in hypertensive men with erectile dysfunction: results of a pilot study

Piha¹,

Kaaja

2003

Int J Impot Res

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Centrally acting (moxonidine) and peripherally acting (metoprolol) sympatholytic agents might have different actions upon penile circulation in hypertensive men with erectile dysfunction. A total of 11 nonsmoking, hypertensive but otherwise healthy men with erectile dysfunction were studied after 8 weeks on moxonidine monotherapy (0.4 mg per day, increased to 0.6 mg if needed) and then after 8 weeks of metoprolol monotherapy (100 mg per day, increased to 200 mg if needed) in a crossover design. At the end of each treatment phase, the subjects were asked about their subjective erectile capacity (nocturnal and coital erections), and resting and stimulated (after intracavernosal injection of a mixture of alprostadil and phentolamine) penile deep artery diameters and systolic peak velocities were measured by color Doppler ultrasonography. There were no significant differences in blood pressure after either therapy. The change from earlier antihypertensive therapy, moxonidine produced significant subjective amelioration of sexual dysfunction in 9/11 of the men (Po0.001), whereas 9/11 returned to impaired dysfunction after crossover to metoprolol treatment. Resting and stimulated deep penile diameters and peak systolic velocities were higher after moxonidine treatment compared with metoprolol (diameters: Po0.004, Po0.0001; velocities: Po0.008, Po0.038). The centrally acting sympatholytic agent moxonidine seems to improve erectile function both subjectively and objectively and has a better effect on penile circulation compared with the peripherally acting sympatholytic agent metoprolol.

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“…A ativação desses receptores no VLM demonstrou reduzir a atividade do sistema nervoso simpático e, assim, diminuir a PA 8,9 , sugerindo que o efeito hipotensor da moxonidina decorra, preferencialmente, da ação nesses receptores I 1 bulbares, causando uma diminuição do tônus simpático 6 e da resistência vascular periférica (RVP) ( fig. 1) 5,[10][11][12][13] . Esta afinidade é muito maior com os receptores imidazolínicos do que com os a 2 adrenérgicos 14 , sendo descritas diferenças entre 40 5 e 600 vezes 14 .…”

Section: Aspectos Farmacodinâmicosunclassified

Moxonidina. Um novo anti-hipertensivo de ação central

Leães¹,

Rosito

1998

Arq. Bras. Cardiol.

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Pharmacology of Moxonidine, an I1-Imidazoline Receptor Agonist

Cited by 62 publications

References 120 publications

The effect of moxonidine on feeding and body fat in obese Zucker rats: role of hypothalamic NPY neurones

The effect of moxonidine on feeding and body fat in obese Zucker rats: role of hypothalamic NPY neurones

Effects of moxonidine and metoprolol in penile circulation in hypertensive men with erectile dysfunction: results of a pilot study

Moxonidina. Um novo anti-hipertensivo de ação central

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