Receptors in the gastrointestinal tract

Bertaccini, G.; Coruzzi, Gabriella

doi:10.1016/0031-6989(87)90001-4

Cited by 13 publications

(17 citation statements)

References 42 publications

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“…It acts further through receptors of the muscarinic type, which are no longer considered as a homogenous population and were first divided into M| and M2 receptors. This differentiation has been achieved mainly by pharmacological characterization with two compounds, the selective M, ago nist McNA 343 and the selective M, antago nist pirenzepine [1,4], M, receptors are believed to be located in ganglia, whereas M2 receptors are found on nerve terminals and peripheral effector cells like smooth muscle, glands and enterocytes [5]. The concentration of M) receptors in the small intestine appears to present only about '/ ioth of the total concentration of choliner gic receptors [6],…”

Section: Cholinergic-receptor Subtypes and Their Cellular Localizationmentioning

confidence: 99%

“…From the controversal data, only two findings will be mentioned here: (1) Whereas the therapeutic value of adreno ceptor agonists and antagonists is clearly es tablished in cardiovascular or respiratory diseases, none of the drugs can be considered as a therapeutic tool in motility disorders. The following paragraph deals with com pounds under clinical consideration.…”

Section: Adrenergic-receptor-mediated Functionmentioning

confidence: 99%

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Gastrointestinal Receptors and Drugs in Motility Disorders

Ruoff

Fladung²,

Demol³

et al. 1991

Digestion

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The review describes gastrointestinal receptors which are of therapeutic interest for the treatment of motility disorders. It updates the present knowledge on muscarinic, adrenergic, dopamine, opioid and dihydropyridine receptors, their subtypes, cellular sites and functional role as drug targets. On the basis of this pharmacological receptor concept, drugs like bethanechol, clonidine, lidamidine, metoclopramide, domperidone, cisapride, loperamide and nifedipine are evaluated in proven and potential indications. In view of the very complex regulation of motility, our understanding of receptors is still fragmentary and our tools to treat motility disorders do not fulfil all therapeutic requirements. This review tries to point out the areas of particular need for further basic research and the prospects of further drug development.

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Section: Cholinergic-receptor Subtypes and Their Cellular Localizationmentioning

confidence: 99%

Section: Adrenergic-receptor-mediated Functionmentioning

confidence: 99%

Gastrointestinal Receptors and Drugs in Motility Disorders

Ruoff

Fladung²,

Demol³

et al. 1991

Digestion

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“…However, as stated by Bertaccini and Coruzzi [5], the fact that peripheral antagonists like domperidone [63] may increase gut motility can be considered as pharmacological evidence for the presence of dopamine receptors in the gastrointestinal tract. Figure 2 shows the typical effects of dopamine, Prokinetic drugs: metoclopramide, domperidone, cisapride.…”

Section: Doparnine Receptors and Prokinetic Drugsmentioning

confidence: 99%

“…Recent discoveries have shown that nearly all receptors exist in several forms for which specific agonistic or antagonistic drugs have been found [5]. The exact importance of some of the gut receptors is still unknown.…”

Section: Nervous Control and Gastrointestinal Receptorsmentioning

confidence: 99%

“…Adrenergic receptors are activated by norepinephrine and are more recently classified into 4 subtypes, c~1, c~2,/31 and/32, c~1, /31 and B2 are essentially located postsynaptically on the effector organs whereas c~2-receptors are located presynaptically regulating ACh release from cholinergic neurons of the myenteric plexuses [5]. The major role of adrenergic receptors in gut motility is relaxation, especially by regulating the release of neurotransmitters like ACh from the intrinsic nerves.…”

Section: Adrenergic Receptors and Specific Drugsmentioning

confidence: 99%

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Rational pharmacotherapy of gastrointestinal motility disorders

1989

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Nervous control of gastrointestinal motility is extremely complex, is regulated by the enteric system, the "brain of the gut", and modulated by extrinsic nerves. This system with its multiplicity of transmitters and receptors does not always allow a clear interpretation of experimental data, especially with compounds lacking specificity. In this review the complex situation is described particularly in relation to receptor populations (cholinergic, adrenergic, dopamine, histamine, 5-hydroxytryptamine, opioid, gamma-aminobutyric acid (GABA), prostanoid and dihydropyridine receptors), therapeutic aspects of drugs and their usefulness in children. Newer principles with known drugs and promising new compounds with a more appropriate kinetic or fewer side-effects, deriving from distinct pharmacological groups, as candidates for the treatment of gastrointestinal disorders are considered e.g. anticholinergics (prifinium or actilonium bromide), adrenergic alpha 2-agonists (clonidine, lidamidine) for diarrhoea in diabetic neuropathy, adrenergic beta-blockers for shortening postoperative ileus (propranolol), dopamine receptor antagonists (metoclopramide, domperidone, alizapride) and another prokinetic substance (cisapride) which may be useful for a number of applications as gastro-oesophageal reflux, gastro-paresis, intestinal pseudo-obstruction, cystic fibrosis and constipation, morphine derivatives (e.g. loperamide) for intractable diarrhoea and calcium antagonists (e.g. nifedipine) for achalasia. Increasing experience in digestive tract pharmacology and reliable clinical studies will furthermore be the basis for a more specific and better tolerated therapy of gastrointestinal motility disorders in adults and children.

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Prokinetic agents for lower gastrointestinal motility disorders

Longo

Vernava

1993

Diseases of the Colon &Amp; Rectum

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Prokinetic agents are currently being investigated as potential therapies for motility disorders of the lower gastrointestinal tract. Cholinergic agonists such as bethanechol are known to improve postoperative ileus but are limited because of side effects. Dopamine antagonists such as domperidone appear to have maximal prokinetic effect in the proximal gastrointestinal tract and are effective for such conditions as gastroparesis and gastroesophageal reflux, but they appear to have little physiologic effect in the colon or in colonic motility disorders. Naloxone, an opioid antagonist, appears to hold promise in patients with irritable bowel syndrome, small intestinal pseudo-obstruction, and constipation. Erythromycin exerts its prokinetic effect by acting as a motilin agonist; it has been used in the treatment of diabetic gastroparesis and appears to improve symptoms of colonic pseudo-obstruction and postoperative ileus. Metoclopramide, a combined cholinergic agonist and dopamine antagonist, is currently used exclusively for proximal motility dysfunction. Cisapride appears to hold the most promise for patients with colonic motility disorders. In patients with postoperative ileus, cisapride is associated with an increased return of bowel function compared with placebo. In patients with chronic constipation, cisapride increases stool frequency and decreases laxative abuse in both adults and children. Hopefully, as an understanding of gastrointestinal motility increases, effective prokinetic agents will be developed that will improve symptoms of patients with large bowel motility disorders and may also help to predict those patients who benefit from surgical management for constipation.

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Receptors in the gastrointestinal tract

Cited by 13 publications

References 42 publications

Gastrointestinal Receptors and Drugs in Motility Disorders

Gastrointestinal Receptors and Drugs in Motility Disorders

Rational pharmacotherapy of gastrointestinal motility disorders

Prokinetic agents for lower gastrointestinal motility disorders

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