PMID: 7085409Apr 1, 1982Paper

The muscarinic receptors of airway smooth muscle: their characterization in vitro

Journal of Applied Physiology: Respiratory, Environmental and Exercise Physiology
C MurlasJ M Roberts


We have used radioligand binding and in vitro muscle contraction techniques to characterize the muscarinic cholinergic receptors of canine tracheal smooth muscle. The tritiated muscarinic antagonist, quinuclidinyl benzilate ([3H]QNB), bound no particulate preparations of tracheal smooth muscle with high affinity, saturability, pharmacologic specificity, and stereoselectivity. The equilibrium dissociation constant for the binding reaction was 33 +/- 3 pM (mean +/- SE). The concentration of binding sites was 410 +/- 34 pmol/g protein. The ability of muscarinic agents to inhibit [3H]QNB binding paralleled their relative effects on tracheal smooth muscle contraction in vitro. We found the anesthetic agents, lidocaine and tetracaine, and the nicotonic cholinergic antagonist d-tubocurarine, were competitive inhibitors of [3H]QNB binding to the tracheal smooth muscle preparations. Histamine, aminophylline, and adrenergic agonists did not act as competitive inhibitors. The guanine nucleotide, guanyl-5'-imidodiphosphate, reduced the ability of the muscarinic agonist, acetylcholine, to compete with high affinity for [3H]QNB binding site(s) in tracheal smooth muscle but had minimal effects on the binding of the muscarinic antagonist, atro...Continue Reading


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Related Concepts

Acetylcholine Sulfate (1: 1)
Canis familiaris
Guanylyl Imidodiphosphate
Hydrogen-Ion Concentration
Muscle Proteins
Smooth Muscle
Quinuclidinyl Benzilate
Cholinergic Receptors

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