Anti-obesity drugs: A critical review of current therapies and future opportunities

Pharmacology and Therapeutics

Volumn 89, Issue 1, 2001, Pages 81-121

  Clapham, John C ^a   Arch, Jonathan R S ^b   Tadayyon, Mohammad ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Tel: +44 1279 627061 ^*

Author keywords

Energy expenditure; Feeding peptides; Gastrointestinal peptides; Obesity; Orlistat; Sibutramine

Indexed keywords

1 NAPHTHALENESULFONIC ACID [4 [(4 AMINO 2 QUINAZOLINYLAMINO)METHYL]CYCLOHEXYLMETHYL]AMIDE; AMFEBUTAMONE; AMFEPRAMONE; ANANDAMIDE; DEXFENFLURAMINE; DIMAPRIT; FENFLURAMINE; FLUOXETINE; GALANIN; GR 231118; HISTAMINE; HISTAMINE H1 RECEPTOR ANTAGONIST; HISTAMINE H3 RECEPTOR ANTAGONIST; J 104870; L 152804; LY 35797; MAZINDOL; MELANIN CONCENTRATING HORMONE; N2 DIPHENYLACETYL N (4 UREIDOMETHYLBENZYL)ARGININAMIDE; NALPHA (DIPHENYLACETYL) N (4 HYDROXYBENZYL) DEXTRO ARGININAMIDE; NEUROPEPTIDE Y; NEUROPEPTIDE Y RECEPTOR ANTAGONIST; PHENTERMINE; PHENYLPROPANOLAMINE; RIMONABANT; SERTRALINE; SIBUTRAMINE; SR 120562A; TOPIRAMATE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

DROWSINESS; DRUG MECHANISM; DRUG STRUCTURE; HUMAN; LIPID ABSORPTION; NONHUMAN; OBESITY; PRIORITY JOURNAL; REVIEW; VALVULAR HEART DISEASE;

ANIMALS; ANTI-OBESITY AGENTS; ENERGY METABOLISM; FORECASTING; HUMANS; OBESITY;

EID: 0035064737     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0163-7258(00)00105-4     Document Type: Review

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233. Structure and function of the uncoupling protein from brown adipose tissue
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256. The receptor for the orexigenic peptide melanin-concentrating hormone is a G-protein-coupled receptor
257. Molecular pharmacological aspects of histamine receptors
258. Metabolic consequences of fenfluramine for the control of body weight
259. Leptin receptor activation of SH2 domain containing protein tyrosine phosphatase 2 modulates Ob receptor signal transduction
260. Bombesin reduces food intake in lean man by a cholecystokinin-independent mechanism
261. Obese women are less sensitive for the satiety effects of bombesin than lean women
262. Plasma cholecystokinin and pancreatic polypeptide secretion in response to bombesin, meal ingestion and modified sham feeding in lean and obese persons
263. The sleep disorder canine narcolepsy is caused by a mutation in the hypocretin (orexin) receptor 2 gene
264. Structural requirements for the biological activity of enterostatin
265. Enterostatin actions in the amygdala and PVN to suppress feeding in the rat
266. Changes in the microstructure of feeding after administration of enterostatin into the paraventricular nucleus and the amygdala
267. Familial predisposition for obesity may modify the predictive value of serum leptin concentrations for long-term weight change in obese women
268. Contribution of β3-adrenoceptor activation to ephedrine-induced thermogenesis in humans
269. Cloning and functional expression of the human histamine H3 receptor
270. Agouti protein is an antagonist of the melanocyte-stimulating-hormone receptor
271. Independent feeding and metabolic actions of orexins in mice
272. Melanin-concentrating hormone, a functional melanocortin antagonist in the hypothalamus
273. Sibutramine, a serotonin-norepinephrine reuptake-inhibitor for the treatment of obesity
274. Attenuation of the anorectic effects of glucagon, cholecystokinin, and bombesin by the amylin receptor antagonist CGRP(8-37)
275. The histaminergic, but not the serotoninergic, system mediates amylin's anorectic effect
276. Ultrastructure of bombesin-like immunoreactive nerve terminals in the nucleus of the solitary tract and the dorsal motor nucleus
277. Zucker obese rats, defect in brain histamine control of feeding
278. Fluoxitine improves insulin sensitivity in obese patients with non-insulin-dependent diabetes mellitus independently of weight loss
279. Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors
280. Intraventricular injection of neuropeptide Y antisera curbs weight gain and feeding, and increases the display of sexual behaviors in obese Zucker female rats
281. Response of melanocortin-4 receptor-deficient mice to anorectic and orexigenic peptides
282. Role of the Y5 neuropeptide Y receptor in feeding and obesity
283. Discovery and characterization of endogenous cannabinoids
284. Cannabinoids and appetite stimulation
285. The use of selective serotonin reuptake inhibitors in eating disorders
286. Bombesin, potential integrative peptide for feeding and satiety
287. Burden of illness review of obesity: Are the true costs realised?
288. Sibutramine. A review of its contribution to the management of obesity
289. Repeated intracerebroventricular administration of glucagon-like peptide-1-(7-36) amide or exendin-(9-39) alters body weight in the rat
290. Effect of enterostatin given intravenously and intracerebroventricularly on high-fat feeding in rats
291. Metabolic effects of galanin injections into the paraventricular nucleus of the hypothalamus
292. Does the histaminergic system mediate bombesin/GRP-induced suppression of food intake
293. Rapid alterations of hypothalamic and hippocampal bombesin-like peptide levels with feeding status
294. Regulation of body weight in seasonal animals
295. Regulation of galanin gene expression in the hypothalamic paraventricular nucleus of the obese Zucker rat by manipulation of dietary macronutrients
296. Capsaicin-sensitive fibers are required for the anorexic action of systemic but not central bombesin
297. Stimulation of energy expenditure by LY377604, a beta3-adrenergic receptor agonist with beta1/2-antagonist properties, in healthy male subjects
298. Cloning of the mouse agouti gene predicts a secreted protein ubiquitously expressed in mice carrying the lethal yellow mutation
299. Semiquantitative distribution of galanin-receptor (Gal-R1) mRNA-containing cells in the male rat hypothalamus
300. Hypothalamic proopiomelanocortin messenger-RNA is reduced by fasting in ob/ob and db/db mice, but is stimulated by leptin
301. Both amidated and nonamidated forms of glucagon-like peptide I are synthesized in the rat intestine and the pancreas
302. Congenital leptin deficiency is associated with severe early-onset obesity in humans
303. Biochemical localization and characterization of bombesin-like peptides in discrete regions of rat brain
304. The NPY Y1 receptor antagonist BIBP 3226 blocks NPY induced feeding via a non-specific mechanism
305. Neurons containing orexin in the lateral hypothalamic area of the adult rat brain are activated by insulin-induced acute hypoglycemia
306. Involvement of the histaminergic system in leptin-induced suppression of food intake
307. Localization of the melanocortin-4 receptor (MC4-R) in neuroendocrine and autonomic control circuits in the brain
308. Obesity, diabetes and functions for proopiomelanocortin-derived peptides
309. The yellow mouse obesity syndrome and mechanisms of agouti-induced obesity
310. Melanocortin mediated inhibition of feeding behavior in rats
311. Intravenous infusion of bombesin reduces food intake in humans
312. Uncoupling protein 3: Its possible biological role and mode of regulation in rodents and humans
313. Expression of uncoupling protein in skeletal muscle and white fat of obese mice treated with thermogenic beta 3-adrenergic agonist
314. Effects of FL-386 on faecal lipid excretion in humans
315. Normal feeding behaviour, body weight and leptin response require the neuropeptide Y Y2 receptor
316. 3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides
317. A role for uncoupling protein-2 as a regulator of mitochondrial hydrogen peroxide generation
318. Effects of ebelactone B, a lipase inhibitor on intestinal fat absorption in the rat
319. Mice lacking bombesin receptor subtype-3 develop metabolic defects and obesity
320. Functional properties of two bombesin-like peptide receptors revealed by the analysis of mice lacking neuromedin B receptor
321. Chronic effects of intracerebral ventricular enterostatin in Osborne-Mendel rats fed a high-fat diet
322. Differential inhibition of fat intake in two strains of rat by the peptide enterostatin
323. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein
324. Hypothalamic sites of neuronal histamine action on food intake by rats
325. Glucagon-like peptides GLP-1 and GLP-2, predicted products of the glucagon gene, are secreted separately from pig small intestine but not pancreas
326. Glucagon-like peptide I receptors in the subfornical organ and the area postrema are accessible to circulating glucagon-like peptide I
327. Insatiable feeding evoked in rats by recurrent perfusion of neuropeptide Y in the hypothalamus
328. Histochemistry and function of bombesin-like peptides
329. Neuronal location of the bombesin-like immunoreactivity in the central nervous system of the rat
330. Clinical aspects of ephedrine in the treatment of obesity
331. Hypothalamic neuropeptide Y and galanin in overweight rats fed a cafeteria diet
332. Cardiovascular response, feeding behaviour and locomotor activity in mice lacking the NPY Y1 receptor
333. Weight loss in patients receiving tiporamate for intractable epilepsy
334. Neurons containing hypocretin (orexin) project to multiple neuronal systems
335. Topiramate reduces energy gain in lean and obese Zucker rats
336. Pharmacological characteristics and species-related variations of beta 3-adrenergic receptors
337. The novel neuropeptide, orexin-A, modulates the sleep-wake cycle of rats
338. ACTH-(1-24) and alpha-MSH antagonize feeding behavior stimulated by kappa opiate agonists
339. Neuropeptide Y receptors mediating feeding in the rat
340. Hyperenterostatinemia in premenopausal obese women
341. Melanin-concentrating hormone is a potent anorectic peptide regulated by food-deprivation and glucopenia in the rat
342. Disruption of neural signaling within the hypothalamic ventromedial nucleus upregulates galanin gene expression in association with hyperphagia, an in situ hybridization analysis
343. A role for melanin-concentrating hormone in the central regulation of feeding behaviour
344. Attenuated GLP-1 secretion in obesity, cause or consequence?
345. Relatively low plasma leptin concentrations precede weight gain in Pima Indians
346. The uncoupling protein homologues, UCP1, UCP2, UCP3, StUCP and AtUCP
347. Characterization of two cloned human CB1 cannabinoid receptor isoforms
348. A galanin-like peptide in the central nervous system and intestine of the rat
349. Sibutramine reduces food intake in non-dieting women with obesity
350. A C-terminal fragment of agouti-related protein increases feeding and antagonizes the effect of alpha-melanocyte stimulating hormone in vivo
351. Melanin-concentrating hormone acutely stimulates feeding, but chronic administration has no effect on body weight
352. Intravenous enterostatin does not affect single meal food intake in man
353. Weight loss, weight maintenance, and improved cardiovascular risk factors after 2 years treatment with orlistat for obesity
354. Impaired processing of brain proneurotensin and promelanin-concentrating hormone in obese fat/fat mice
355. Pharmacology and intracellular mechanisms of the native human orphan receptor BRS-3 in lung cancer cells
356. Changes in plasma insulin, enterostatin and lipoprotein levels during an energy-restricted dietary regimen including a new oat-based liquid food
357. Evidence suggesting that galanin (GAL), melanin-concentrating hormone (MCH), neurotensin (NT), propiomelanocortin (POMC) and neuropeptide Y (NPY) are targets of leptin signaling in the hypothalamus
358. Molecular characterization of the melanin-concentrating-hormone receptor
359. Feeding induced by blockade of histamine H1-receptor in rat brain
360. Hypothalamic neuronal histamine - Implications of its homeostatic control of energy metabolism
361. Orexins and orexin receptors - A family of hypothalamic neuropeptides and G-protein coupled receptors that regulate feeding behaviour
362. A 35 amino acid fragment of leptin inhibits feeding in the rat
363. Inhibition of food intake by neuropeptide Y Y5 receptor antisense oligodeoxynucleotides
364. Neuropeptide Y Y1 receptor antisense oligodeoxynucleotides enhance food intake in energy-deprived rats
365. Effect of galanin on food intake in rats, involvement of lateral and vetromedial hypothalamic sites
366. Inhibition of noradrenaline release in the rat brain cortex via presynaptic H3 receptors
367. Dissociation of serum leptin concentration and body fat content during long term dietary intervention in obese individuals
368. Leptin increases hypothalamic POMC mRNA expression in the rostral arcuate nucleus
369. Central nervous system control of food intake
370. Glucose intolerance but normal satiety in mice with a null mutation in the glucagon-like peptide 1 receptor gene
371. -/- mice
372. Effects of sibutramine on resting metabolic rate and weight loss in overweight women
373. 3-adrenoceptor agonists of differing selectivities
374. Effects of glucagon-like peptide 1 (7-36 amide) on whole-body protein metabolism in healthy man
375. Injection of anti-neuropeptide Y γ-globulin into the hypothalamic paraventricular nucleus decreases food intake in rats
376. Mice lacking melanin-concentrating hormone are hypophagic and lean
377. Glucagon-like peptide-1 receptor (GLP1-R) mRNA in the rat hypothalamus
378. Hypothalamic expression of ART, a novel gene related to agouti, is up-regulated in obese and diabetic mutant mice
379. SR 141716, a CB1 cannabinoid receptor antagonist, selectively reduces sweet food intake in marmoset
380. Overexpression of muscle uncoupling protein 2 content in human obesity associates with reduced skeletal muscle lipid utilization
381. The effects of leptin on REM sleep and slow wave delta in rats are reversed by food deprivation
382. Randomised placebo-controlled trial of orlistat for weight loss and prevention of weight regain in obese patients
383. Immunocytochemical mapping of galanin-like neurones in the rat central nervous system
384. Characterization of recombinant human orexin receptor pharmacology in a Chinese hamster ovary cell-line using FLIPR
385. Chronic cerebroventricular galanin does not induce sustained hyperphagia or obesity
386. Expression cloning of a rat hypothalamic galanin receptor coupled to phosphoinositide turnover
387. BRL 35135, an orally active antihyperglycaemic agent with weight reducing effects
388. Effect of central injection of anti-orexin 1 receptor antibody on food intake in rats
389. The human uncoupling protein-3 gene - Genomic structure, chromosomal localization, and genetic basis for short and long form transcripts
390. Neurochemical interactions in the control of ingestive behaviour
391. Glutamate and its receptors in lateral hypothalamic stimulation of eating
392. Repeated hypothalamic stimulation with neuropeptide Y increases daily carbohydrate and fat intake and body weight gain in female rats
393. Neuropeptide Y chronically injected into the hypothalamus, a powerful neuro-chemical inducer of hyperphagia and obesity
394. The perifornical area, the major focus of (a) patchily distributed hypothalamic neuropeptide Y-sensitive feeding system(s)
395. Altered gene expression in striatal projection neurons in CB1 cannabinoid receptor knockout mice
396. Uncoupling protein 2 from carp and zebrafish, ectothermic vertebrates
397. 3-adrenergic receptor agonist for treating obesity and diabetes
398. Multiple neuropeptide Y receptors regulate K+ and Ca2+ channels in acutely isolated neurons from the rat arcuate nucleus
399. Feeding response to central orexins
400. Galanin - A novel biologically active peptide from porcine intestine
401. Effects of PVN galanin on macronutrient selection
402. Regulation of hypothalamic POMC mRNA by leptin in ob/ob mice
403. Differences between the effects of noradrenaline and the β-adrenoceptor agonist BRL 28410 in brown adipose tissue and hind limb of the anaesthetized rat
404. A small, nonpeptidyl mimic of granulocyte-colony-stimulating factor
405. 3-agonist ZD2079 stimulates 24-hour energy expenditure through increased fidgeting. A 14 day, randomized placebo-controlled study in obese subjects
406. Randomised comparison of diets for maintaining obese subjects' weight after major weight loss: Ad lib, low fat, high carbohydrate diet v fixed energy intake
407. Safety and efficacy of long-term treatment with ephedrine, caffeine and an ephedrine/caffeine mixture
408. 3-adrenoceptor agonists BRL 35135A and ZD2079
409. Two important systems in energy homeostasis: Melanocortins and melanin-concentrating hormone
410. The obese phenotype of melanin concentrating hormone overexpressing mice
411. Functional interactions between melanin-concentrating hormone, neuropeptide Y, and anorectic neuropeptides in the rat hypothalamus
412. A beta-3 adrenergic agonist (BRL-37344) decreases food intake
413. Antidiuresis induced by infusions of histamine into the brain ventricles of conscious hydrated goats
414. A role of glucagon-like peptide-1 in the central regulation of feeding
415. Trp64Arg mutation of beta(3)-adrenoceptor gene deteriorates lipolysis induced by beta(3)-adrenoceptor agonist in human omental adipocytes
416. A frameshift mutation in human MC4R is associated with a dominant form of obesity
417. Leptin activation of Stat3 in the hypothalamus of wild-type and ob/ob but not db/db mice
418. Hypothalamic hypocretin (orexin): Robust innervation of the spinal cord
419. Metabolic, gastrointestinal, and CNS neuropeptide effects of brain leptin administration in the rat
420. Central infusions of leptin and GLP-1-(7-36) amide differentially stimulate c-FLI in the rat brain
421. Glucagon-like peptide-1 and satiety
422. The beneficial effects of modest weight loss on cardiovascular risk factors
423. Direct effects of ephedrine isomers on human beta-adrenergic receptor subtypes
424. 2 release by mitochondria from rat skeletal muscle
425. 4 receptor antagonist (HS014) on melanocortin-induced behavioral effects in rats
426. UCP3 - An uncoupling protein homologue expressed preferentially and abundantly in skeletal muscle and brown adipose tissue
427. The effect of orlistat on the fatty acid composition of serum lipid fractions in obese subjects
428. Increase in uncoupling protein-2 mRNA expression by BRL49653 and bromopalmitate in human adipocytes
429. Modulation of anxiety and neuropeptide Y-Y1 receptors by antisense oligodeoxynucleotides
430. The effect of sibutramine on resting energy expenditure and adrenaline-induced thermogenesis in obese females
431. Cardiovascular effects of ephedrine, caffeine and yohimbine measured by thoracic electrical bioimpedance in obese women
432. Hypothalamic galanin, control by signals of fat metabolism
433. Interactions between leptin and hypothalamic neuropeptide Y neurons in the control of food intake and energy homeostasis in the rat
434. Molecular cloning and functional characterization of a new galanin receptor subtype
435. Cloning and expressional characterization of a novel galanin receptor
436. Fluoxetine-maintained obese humans, effect on food intake and body weight
437. Intraventricular administration of enterostatin decreases food intake in baboons
438. Lipstatin, an inhibitor of pancreatic lipase, produced by Streptomyces toxytricini, I. Producing organism, fermentation, isolation and biological activity
439. Long-term weight control study, conclusions
440. Long-term weight control study. I (weeks 0 to 34). The enhancement of behavior modification, caloric restriction, and exercise by fenfluramine plus phentermine versus placebo
441. Long-term weight control study. IV (weeks 156 to 190). The second double-blind phase
442. Long-term weight control study. II (weeks 34 to 104). An open-label study of continuous fenfluramine plus phentermine versus targeted intermittent medication as adjuncts to behavior modification, caloric restriction, and exercise
443. Long-term weight control study. III (weeks 104 to 156). An open-label study of dose adjustment of fenfluramine and phentermine
444. The pharmacologic approach to the treatment of obesity
445. Synergistic interactions between fenfluramine and phentermine
446. Amidated and non-amidated glucagon-like peptide-1 (GLP-1). non-pancreatic effects (cephalic phase acid secretion) and stability in plasma in humans
447. 3-adrenoceptor agonist in humans
448. β-Adrenoceptor subtypes mediating the metabolic effects of BRL 35135 in man
449. Hypothalamic NPY status during positive energy balance and the effects of the NPY antagonist, BW 1229U91, on the consumption of highly palatable energy-rich diet
450. Subtype selectivity of the novel nonpeptide neuropeptide Y Y1 receptor antagonist BIBO 3304 and its effect on feeding in rodents
451. Increased neuropeptide Y content in individual hypothalamic nuclei, but not neuropeptide Y mRNA, in diet-induced obesity in rats
452. Agouti protein antagonism of melanocortin receptors: Valine83 and proline86 are important binding determinant
453. Anandaminde induces overeating, mediation by central cannabinoid (CB1) receptors
454. 3-adrenoceptor depends on receptor expression level and nature of the assay
455. Substrate supply for thermogenesis induced by the β-adrenoceptor agonist BRL 26830A
456. LY248686, a new inhibitor of serotonin and norepinephrine uptake
457. The pharmacokinetics and acute effects of LY355101, a novel anti-obesity protein, in healthy volunteers
458. Comparison of changes in the extracellular concentration of noradrenaline in rat frontal cortex induced by sibutramine or d-amphetamine, modulation by α2-adrenoceptors
459. Discovery of high affinity bombesin receptor subtype 3 agonists
460. Targeted disruption of the murine galanin gene
461. Stimulation of feeding in lean but not in obese Zucker rats by a selective neuropeptide Y Y5 receptor agonist
462. The pharmacology of neuropeptide Y (NPY) receptor-mediated feeding in rats characterizes better Y5 than Y1, but not Y2 or Y4 subtypes
463. Anorectic effects of the cytokine, ciliary neurotropic factor, are mediated by hypothalamic neuropeptide Y, comparison with leptin
464. Inhibition of food intake by central injection of anti-orexin antibody in fasted rats
465. Down regulation of the prepro-orexin gene expression in genetically obese mice
466. Galanin analogues, agonist and antagonist
467. Composition of weight loss during short-term weight reduction
468. Characterisation of agouti-related protein binding to melanocortin receptors
469. Obesity in the mouse model of pro-opiomelanocortin deficiency responds to peripheral melanocortin
470. A frameshift mutation in MC4R associated with dominantly inherited human obesity
471. Inhibition of neuropeptide Y (NPY)-induced feeding and c-Fos response in magnocellular paraventricular nucleus by a NPY receptor antagonist: A site of NPY action
472. Hypothalamic neuronal histamine as a target of leptin in feeding behavior
473. Cloning of mouse uncoupling protein 3 cDNA and 5′-flanking region, and its genetic map
474. Treatment with orlistat reduces cardiovascular risk in obese patients
475. Positional cloning of the mouse obese gene and its human homologue
476. Discovery of a small molecule insulin mimetic with antidiabetic activity in mice
477. Review of limited systemic absorption of orlistat, a lipase inhibitor, in healthy human volunteers
478. The influence of orlistat on the pharmacokinetics and pharmacodynamics of glyburide in healthy volunteers
479. Long-term systemic exposure of orlistat, a lipase inhibitor, and its metabolites in obese patients