Quinuclidinyl benzilate binding in house fly heads and rat brain.
House fly heads contain a binding site for 3-quinuclidinyl benzilate (QNB) that is quite similar in pharmacology to the muscarinic acetylcholine receptor of vertebrate tissues. The house fly site binds [3H]QNB reversibly with a Kd of 260 pM and Bmax of 1 pmol/g of heads from direct binding measurements. The Kd calculated from the ratio of the dissociation rate constant (2 x 10(-4)sec-1) to the association rate constant (2.5 x 10(6) M-1sec-1) was 80 pM. The house fly site binds (-)quinuclidinyl benzilate preferentially, as do classic muscarinic receptors. The binding is also sensitive to other muscarinic antagonists and agonists. Nicotinic and other drugs are no more effective on the house fly site than they are on the rat brain muscarinic receptor itself. These binding studies suggest that the house fly QNB binding site is a muscarinic receptor.
D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D006793:Houseflies / Q000378:metabolism*; D007700:Kinetics; D010600:Pharmacology; D011812:Quinuclidines / Q000378:metabolism*; D011813:Quinuclidinyl Benzilate / Q000378:metabolism*; D051381:Rats; D011950:Receptors, Cholinergic / Q000378:metabolism*; D011976:Receptors, Muscarinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011812:Quinuclidines; D011950:Receptors, Cholinergic; D011976:Receptors, Muscarinic; C028484:quinuclidinyl benzilate receptor; D011813:Quinuclidinyl Benzilate