Receptors cholinergic

FIGURE 14.5 The autonomic nervous system innervates smooth muscle, cardiac muscles, and gland. ACh = acetylcholine N = nicotinic cholinergic receptors M = muscarinic cholinergic receptors S = sympathetic chain P = parasympathetic chain E = epinephrine D = dopamine NE = norepinephrine Sup. = superior Inf. = inferior. 

Acetylcholine receptors are classified as either muscarinic cholinergic receptors or nicotinic cholinergic receptors. The alkaloid muscarine mimics the effects produced by stimulation of the parasympathetic system. These effects are postganglionic and are exerted on exocrine glands, cardiac muscle, and smooth muscle. The alkaloid nicotine mimics the actions of acetylcholine, which include stimulation of all autonomic ganglia, stimulation of the adrenal medulla, and contraction of skeletal muscle. 

Dimethylphenylpiperazinium stimulates the autonomic ganglia, tetraethylammonium and hexamethonium block the autonomic ganglia, phenyltrimethylammonium stimulates skeletal motor muscle end plates, decamethonium produces neuromuscular blockade, and zZ-tubocurarine blocks both the autonomic ganglia and the motor fiber end plates. 

Among the agents cited, only d-tubocurarine is useful as a drug (skeletal muscle relaxant) the rest are useful only as research tools. Cholinesterase, found in liver and plasma, can hydrolyze other esters such as succinylcholine (a skeletal muscle relaxant). Cholinergic peripheral receptors are located on (1) postganglionic parasympathetic fibers, (2) postganglionic sympathetic fibers, (3) all autonomic ganglia, and (4) skeletal end plates. 

Slight cardiac slowing some dryness of mouth inhibition of sweating 

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Nicotinic Receptor Agonists. There has been significant activity in the development of muscarinic cholinergic receptor agonists for dementia. In addition, agents that interact with nicotinic cholinergic receptors may also have therapeutic value. Nicotinic receptors have been reported to be... 

Acetyl choline is the natural neurotransmitter for the cholinergic receptor. Two distinct receptor subtypes have been characterized based on their binding affinity for either nicotine (189) and (190) or muscarine (191). 

In contrast to all this negativity, it must be acknowledged that more is known about the structure and function of cholinergic receptors and synapses, especially the nicotinic ones, than for the receptors of any other NT. It is unfortunate that nicotinic synapses are not very common in the CNS. 

Many drugs bind to cholinergic receptors but few of them enter the brain and those that do are not noted for their effects. 

Ward, D., and Trevor, A. Phencyclidine-induced alteration in rat muscarinic cholinergic receptor regulation. ux U Pharmacol 74 189-193, 1981. 

Motion sickness is caused by stimulation of the vestibular system. This area contains many histaminic (Hj) and muscarinic cholinergic receptors. The higher brain (i.e., cerebral cortex) is affected by sensory input such as sights, smells, or emotions that can lead to vomiting. This area is involved in anticipatory nausea and vomiting associated with chemotherapy. 

Antihistamines are commonly used to prevent and treat nausea and vomiting due to motion sickness, vertigo, or migraine headache.1,17 Their efficacy is presumably due to the high concentration of histamine (Hx) and muscarinic cholinergic receptors within the vestibular system. Similarly to scopolamine, antihistamines such as diphenhydramine and... 

Monoamine oxidase inhibition Serotonin reuptake inhibition Norepinephrine reuptake inhibition Dopamine reuptake inhibition a2-Adrenergic receptor blockade Serotonin-2A receptor blockade Serotonin-2C receptor blockade Serotonin-3 receptor blockade op-Adrenergic receptor blockade Histamine-1 receptor blockade Muscarinic cholinergic receptor blockade... 

Gronier, B. Rasmussen, K. (1998). Activation of midbrain presumed dopaminergic neurones by muscarinic cholinergic receptors an in vivo electrophysiological study in the rat. Br. J. Pharmacol. 124, 455-64. 

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