Comprehensive Physiology Wiley Online Library

Pharmacology of drugs acting on gastrointestinal motility

Full Article on Wiley Online Library



Abstract

The sections in this article are:

1 Nature and Classification of Receptors
1.1 Basis of Classification
1.2 Functional Studies of Receptors
1.3 Ligand Binding Studies of Receptors
1.4 Problems in Locus, Classification, and Functional Coupling of Receptors
1.5 Methods of Quantitation of Drug‐Receptor Responses
2 Agents that Act Directly on Postreceptor Mechanisms
3 Isolated Smooth Muscle Cell Preparations for Studying Pharmacology of Gastrointestinal Motility
4 Muscarinic Receptors
4.1 Muscarinic Receptor Subtypes
4.2 Locus of Action of Muscarinic Receptors
4.3 Modulation of Muscarinic Receptor
4.4 Muscarinic Postreceptor Events
4.5 Therapeutic Application of Muscarinic Pharmacology
5 Adrenergic Receptors and Gut Motility
5.1 Sympathetic Pathways
5.2 Functions of Adrenergic Innervation
5.3 Receptor Classification
5.4 Postreceptor Mechanisms
5.5 β‐Adrenoceptor‐Mediated Mechanisms
6 Serotonin Receptors and Gut Motility
6.1 Introduction
6.2 Locus and Function of Serotonin Nerves
6.3 Classification of Serotonin Receptors
6.4 Direct Action on Smooth Muscle
6.5 Actions of Serotonin on Enteric Nerves
6.6 Therapeutic Considerations
7 Purinergic Receptors and Gut Motility
7.1 Possible Functions of Purinergic Substances
7.2 Role of Purinergic Substances in Nonadrenergic Inhibition of Gut
7.3 Postsynaptic Activity
7.4 Presynaptic Activity
7.5 Classification
7.6 Mechanisms of Postsynaptic Activity
Figure 1. Figure 1.

Contraction and binding to gastric smooth muscle preparations by carbachol. Relationships between ability of muscarinic agonist carbachol to induce contraction of isolated muscle cells (open circles) and to increase frequency (open triangles) and amplitude (open inverted triangles) of phasic contraction of muscle strips from canine gastric corpus circular muscle. Data are compared with abilities of carbachol to inhibit [3H]quinuclidinyl benzilate (QNB) binding to muscle cells (closed circles) and plasma membranes (closed triangles) prepared from circular muscle of canine gastric corpus.

Adapted from Collins and Crankshaw
Figure 2. Figure 2.

Muscarinic receptors are located on extrinsic nerves of parasympathetic [A ] and sympathetic [B ] nervous systems. They are also located on myenteric ganglia [C ], cholinergic inhibitory nerves [D1], adrenergic inhibitory nerves [D2], and noncholinergic, nonadrenergic inhibitory nerves [D3] of intrinsic nervous system, as well as on smooth muscle [E ]. (+), Indicates excitatory or facilitatory muscarinic receptor; (−), indicates inhibitory muscarinic receptor.



Figure 1.

Contraction and binding to gastric smooth muscle preparations by carbachol. Relationships between ability of muscarinic agonist carbachol to induce contraction of isolated muscle cells (open circles) and to increase frequency (open triangles) and amplitude (open inverted triangles) of phasic contraction of muscle strips from canine gastric corpus circular muscle. Data are compared with abilities of carbachol to inhibit [3H]quinuclidinyl benzilate (QNB) binding to muscle cells (closed circles) and plasma membranes (closed triangles) prepared from circular muscle of canine gastric corpus.

Adapted from Collins and Crankshaw


Figure 2.

Muscarinic receptors are located on extrinsic nerves of parasympathetic [A ] and sympathetic [B ] nervous systems. They are also located on myenteric ganglia [C ], cholinergic inhibitory nerves [D1], adrenergic inhibitory nerves [D2], and noncholinergic, nonadrenergic inhibitory nerves [D3] of intrinsic nervous system, as well as on smooth muscle [E ]. (+), Indicates excitatory or facilitatory muscarinic receptor; (−), indicates inhibitory muscarinic receptor.

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Edwin E. Daniel, Stephen M. Collins, Jo‐Ann E. T. Fox, Jan D. Huizinga. Pharmacology of drugs acting on gastrointestinal motility. Compr Physiol 2011, Supplement 16: Handbook of Physiology, The Gastrointestinal System, Motility and Circulation: 715-757. First published in print 1989. doi: 10.1002/cphy.cp060119