Muscarinic receptor subtypes in the rat prostate gland. 1998

W A Lau, and J N Pennefather
Department of Pharmacology, Monash University, Clayton, Vic., Australia.

Muscarinic receptor subtypes mediating carbachol-induced contractions of the rat prostatic smooth muscle were determined. The rank order of potency of muscarinic receptor antagonists in blocking the effects of carbachol was (mean pKB estimates in parentheses): atropine (8.90) >> para-fluorohexahydrosiladifenidol (7.75) > or = hexahydrosiladifenidol (7.62) > methoctramine (6.89) > or = pirenzepine (6.68) > or = himbacine (6.67). The specific binding of [3H]quinuclidinyl benzilate to the rat prostatic homogenates was competitively inhibited by (mean pKi values in parentheses): atropine (8.89) >> hexahydrosiladifenidol (7.86) > para-fluorohexahydrosiladifenidol (7.28) > or = himbacine (7.22) > pirenzepine (6.63) > or = methoctramine (6.38). These profiles, whilst different, indicate the probable involvement of muscarinic M3 receptors in the carbachol-induced contraction.

UI MeSH Term Description Entries
D008297 Male Males
D011467 Prostate A gland in males that surrounds the neck of the URINARY BLADDER and the URETHRA. It secretes a substance that liquefies coagulated semen. It is situated in the pelvic cavity behind the lower part of the PUBIC SYMPHYSIS, above the deep layer of the triangular ligament, and rests upon the RECTUM. Prostates
D011813 Quinuclidinyl Benzilate A high-affinity muscarinic antagonist commonly used as a tool in animal and tissue studies. Benzilate, Quinuclidinyl
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011976 Receptors, Muscarinic One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology. Muscarinic Acetylcholine Receptors,Muscarinic Receptors,Muscarinic Acetylcholine Receptor,Muscarinic Receptor,Acetylcholine Receptor, Muscarinic,Acetylcholine Receptors, Muscarinic,Receptor, Muscarinic,Receptor, Muscarinic Acetylcholine,Receptors, Muscarinic Acetylcholine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D018678 Cholinergic Agents Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of ACETYLCHOLINE, and drugs that affect the survival of cholinergic neurons. The term cholinergic agents is sometimes still used in the narrower sense of MUSCARINIC AGONISTS, although most modern texts discourage that usage. Acetylcholine Agent,Acetylcholine Agents,Cholinergic,Cholinergic Agent,Cholinergic Drug,Cholinomimetic,Cholinomimetics,Muscarinic,Muscarinic Agent,Muscarinic Agents,Nicotinic Agent,Nicotinic Agents,Cholinergic Drugs,Cholinergic Effect,Cholinergic Effects,Cholinergics,Muscarinic Effect,Muscarinic Effects,Muscarinics,Nicotinic Effect,Nicotinic Effects,Agent, Acetylcholine,Agent, Cholinergic,Agent, Muscarinic,Agent, Nicotinic,Agents, Acetylcholine,Agents, Cholinergic,Agents, Muscarinic,Agents, Nicotinic,Drug, Cholinergic,Drugs, Cholinergic,Effect, Cholinergic,Effect, Muscarinic,Effect, Nicotinic,Effects, Cholinergic,Effects, Muscarinic,Effects, Nicotinic

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