Review article: β3‐adrenoceptor agonists—future anti‐inflammatory drugs for the gastrointestinal tract?

The β3‐adrenoceptor is now a recognized sub‐type of β‐adrenoceptor and is the principle adrenoceptor responsible for lipolysis in rat adipocytes. The receptor is also found in the gastrointestinal tract where β3‐adrenoceptor agonists are both spasmolytic and potent inhibitors of experimental non‐steroidal anti‐inflammatory drug (NSAID)‐induced gastric and small intestinal ulcers. There is evidence to suggest that the underlying mechanism of protection involves enhancement of mucosal blood flow, possibly as a result of relaxation of vascular and non‐vascular smooth muscle.

[1]  R. Pounder,et al.  THE β3‐ADRENOCEPTOR AGONIST CL316243 PREVENTS INDOMETHACIN‐INDUCED JEJUNAL ULCERATION IN THE RAT BY REVERSING EARLY VILLOUS SHORTENING , 1996 .

[2]  F. Ponti,et al.  Functional evidence of atypical β3‐adrenoceptors in the human colon using the β3‐selective adrenoceptor antagonist, SR 59230A , 1996 .

[3]  P. Strong,et al.  Comparison of the profiles of agonists as stimulants of the β3‐adrenoceptor in vitro with their gastroprotective effects in the conscious rat , 1996, British journal of pharmacology.

[4]  R. Pounder,et al.  Pre‐ulcerative villous contraction and microvascular induced by indomethacin in the rat jejunum: a detailed morphological study , 1995, Alimentary pharmacology & therapeutics.

[5]  P. Molenaar,et al.  Characterization and localization of atypical β‐adrenoceptors in rat ileum , 1995 .

[6]  T. Horinouchi,et al.  Possible mechanisms of beta-adrenoceptor-mediated relaxation induced by noradrenaline in guinea pig taenia caecum. , 1995, European journal of pharmacology.

[7]  R. Fremeau,et al.  Distribution of β3-adrenoceptor mRNA in human tissues , 1995 .

[8]  A. Crema,et al.  Inhibitory effects of SR 58611A on canine colonic motility: evidence for a role of β3‐adrenoceptors , 1995, British journal of pharmacology.

[9]  P. Molenaar,et al.  Localisation and characterisation of atypical β-adrenoceptors in skeletal muscle and gut , 1995 .

[10]  J. Takala Splanchnic blood flow and multiple organ failure. , 1995, British journal of hospital medicine.

[11]  D. McLaughlin,et al.  Adrenoceptors mediating relaxation to catecholamines in rat isolated jejunum , 1994, British Journal of Pharmacology.

[12]  J. Montastruc,et al.  Beta-3 adrenoceptor-mediated increase in cutaneous blood flow in the dog. , 1994, The Journal of pharmacology and experimental therapeutics.

[13]  R. Beale,et al.  Assessment of splanchnic oxygenation by gastric tonometry in patients with acute circulatory failure. , 1993, JAMA.

[14]  M. Hudson,et al.  Early histological features of small intestinal injury induced by indomethacin , 1993, Alimentary pharmacology & therapeutics.

[15]  K. Kuratani,et al.  Possible involvement of hyperinsulinemia and adrenergic activation in the pathogenesis of indomethacin-induced antral ulcers in nonfasted hamsters and refed rats. , 1992, The Journal of pharmacology and experimental therapeutics.

[16]  M. Nishimura,et al.  Beta-3 adrenergic agonist, BRL-26830A, and alpha/beta blocker, arotinolol, markedly increase regional blood flow in the brown adipose tissue in anesthetized rats. , 1992, Japanese circulation journal.

[17]  C. Torrance,et al.  Gastrointestinal damage associated with the use of nonsteroidal antiinflammatory drugs. , 1992, The New England journal of medicine.

[18]  P. Canfield,et al.  Stimulation of bicarbonate secretion by atypical beta-receptor agonists in rat cecum in vitro. , 1992, European journal of pharmacology.

[19]  H. Jeffery,et al.  Risk factors for necrotising enterocolitis: the influence of gestational age. , 1992, Archives of disease in childhood.

[20]  E. Livingston,et al.  Strong gastric contractions cause mucosal ischemia. , 1991, The American journal of physiology.

[21]  L. Manara,et al.  In vitro inhibition of intestinal motility by phenylethanolaminotetralines: evidence of atypical β‐adrenoceptors in rat colon , 1990, British journal of pharmacology.

[22]  S. Ebara,et al.  Increased Microvascular Permeability and Lesion Formation During Gastric Hypermotility Caused by Indomethacin and 2‐Deoxy‐D‐Glucose in the Rat , 1990, Journal of clinical gastroenterology.

[23]  A. Levi,et al.  Nonsteroidal antiinflammatory drug-induced intestinal inflammation in humans. , 1987, Gastroenterology.

[24]  M. Sennitt,et al.  Atypical beta-adrenoceptor on brown adipocytes as target for anti-obesity drugs. , 1984, Nature.

[25]  M. Sennitt,et al.  The rat lipolytic beta-adrenoceptor: studies using novel beta-adrenoceptor agonists. , 1984, European journal of pharmacology.

[26]  H. H. Harms,et al.  Beta-adrenoceptor studies. III. On the beta-adrenoceptors in rat adipose tissue. , 1974, European journal of pharmacology.

[27]  V. McGovern,et al.  The nature of benign strictures in ulcerative colitis. , 1969, The New England journal of medicine.