Three acetylcholine receptors in Aplysia neurones. 1972

J Kehoe

1. In the pleural ganglion of Aplysia californica, groups of cells were identified that respond differently to an iontophoretic injection of ACh. The anterior neurones are excited by ACh, whereas the medial cells are inhibited. The inhibitory response is biphasic, consisting of a short-latency, rapid component and a longer-latency, slow component. Homologous responses (e.p.s.p.s in the anterior cells and a two-component inhibitory response in the medial cells) are evoked in these same cell groups by stimulation of an identifiable presynaptic neurone.2. The e.p.s.p. and the corresponding ACh potential are completely eliminated by hexamethonium which has no effect on either of the inhibitory potentials. Both the e.p.s.p. and the rapid i.p.s.p. (and the corresponding ACh potentials) are blocked by tubocurarine, dihydro-beta-erythroidine, strychnine and brucine. These drugs have no effect on the slow inhibitory potential, whether elicited synaptically or by ACh injection. The slow response can be selectively blocked by methylxylocholine, tetraethylammonium (TEA), and phenyltrimethylammonium (PTMA). Since the three types of potentials were found to be differentially affected by ACh antagonists, it was concluded that the various responses are due to activation of three different ACh receptors.3. Of the cholinomimetics tested, only carbamylcholine imitates all three actions of ACh. Nicotinic agents, which were shown to activate the two curare-sensitive receptors, have no stimulating effect on the curare-insensitive receptor. This latter receptor can be selectively stimulated by arecoline. The cholinomimetics were shown to have a secondary blocking effect on the receptor(s) they stimulate.4. Muscarine, even at high doses, is ineffective as either a stimulating or a blocking agent on any of the three receptor types. The muscarinelike drugs oxotremorine, methacholine, and pilocarpine have only weak and non-specific cholinomimetic action on these receptors. Their blocking effects are likewise negligible.5. The two curare-sensitive receptors, which are presumably the same as those described by Tauc & Gerschenfeld (1962), respond like vertebrate nicotinic receptors to both cholinomimetics and cholinolytics. The third receptor type, on the other hand, has a unique pharmacological profile. It is unaffected by both nicotine and muscarine, and is blocked neither by curare nor by atropine. Knowing that it can be stimulated by arecoline and blocked by methylxylocholine, TEA and PTMA does not facilitate its incorporation into the classical scheme of cholinergic receptors.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D008738 Methyl Ethers A group of compounds that contain the general formula R-OCH3. Ethers, Methyl
D008974 Mollusca A phylum of the kingdom Metazoa. Mollusca have soft, unsegmented bodies with an anterior head, a dorsal visceral mass, and a ventral foot. Most are encased in a protective calcareous shell. It includes the classes GASTROPODA; BIVALVIA; CEPHALOPODA; Aplacophora; Scaphopoda; Polyplacophora; and Monoplacophora. Molluscs,Mollusks,Mollusc,Molluscas,Mollusk
D009474 Neurons The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM. Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D010277 Parasympathomimetics Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here. Parasympathomimetic Agents,Parasympathomimetic Drugs,Parasympathomimetic Effect,Parasympathomimetic Effects,Agents, Parasympathomimetic,Drugs, Parasympathomimetic,Effect, Parasympathomimetic,Effects, Parasympathomimetic
D010862 Pilocarpine A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. Isopilocarpine,Isoptocarpine,Ocusert,Pilocarpine Hydrochloride,Pilocarpine Mononitrate, (3S-cis)-Isomer,Pilocarpine Nitrate,Pilocarpine, Monohydrochloride, (3S-cis)-Isomer,Salagen,Hydrochloride, Pilocarpine,Nitrate, Pilocarpine
D011950 Receptors, Cholinergic Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology. ACh Receptor,Acetylcholine Receptor,Acetylcholine Receptors,Cholinergic Receptor,Cholinergic Receptors,Cholinoceptive Sites,Cholinoceptor,Cholinoceptors,Receptors, Acetylcholine,ACh Receptors,Receptors, ACh,Receptor, ACh,Receptor, Acetylcholine,Receptor, Cholinergic,Sites, Cholinoceptive
D002217 Carbachol A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS. Carbamylcholine,Carbacholine,Carbamann,Carbamoylcholine,Carbastat,Carbocholine,Carboptic,Doryl,Isopto Carbachol,Jestryl,Miostat,Carbachol, Isopto
D005724 Ganglia Clusters of multipolar neurons surrounded by a capsule of loosely organized CONNECTIVE TISSUE located outside the CENTRAL NERVOUS SYSTEM.
D005731 Ganglionic Stimulants Agents that mimic neural transmission by stimulation of the nicotinic receptors on postganglionic autonomic neurons. Drugs that indirectly augment ganglionic transmission by increasing the release or slowing the breakdown of acetylcholine or by non-nicotinic effects on postganglionic neurons are not included here nor are the nonspecific cholinergic agonists. Stimulants, Ganglionic
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