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Interaction of iodinated quinuclidinyl benzilate enantiomers with M3 muscarinic receptors

Life Sciences, 1994
We examined the interaction of 3-quinuclidinyl-4-iodobenzilate enantiomers, (RR)- and (SS)-IQNB, relatively receptor-active and -inactive, respectively, with M3-muscarinic receptors (mAChRs) in rat parotid acinar cells in vitro. This stereospecific antagonist pair has often been used for in vivo studies of mAChRs.
Y, Hiramatsu, W C, Eckelman, B J, Baum
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Rabbit blastocysts accumulate [3H]quinuclidinyl benzilate in vitro

Molecular Reproduction and Development, 1991
AbstractDay‐6 rabbit blastocysts were able to accumulate [3H]quinuclidinyl benzilate (QNB) from their environment. This accumulation was reduced approximately 50% in the presence of 1.5 × 10−4 M atropine (an accepted antagonist for ligands which bind to muscarinic cholinergic receptors).
M A, Jones, M, Harper
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ChemInform Abstract: Synthesis of 3‐Quinuclidinyl Benzilate Derivatives.

ChemInform, 1990
AbstractThe 4‐bromo‐ and 4‐iodo analogues (VIII) and (XIII) of 3‐quinuclidinyl benzilate (QNB) are synthesized from the 4‐halobenzophenones (I) as shown in the reaction scheme via O‐silyl cyanohydrins and benzilic acids.
G. W. KABALKA, S. B. MATHUR, Y.‐Z. GAI
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3-Quinuclidinyl Benzilate

2000
Abstract 3-Quinuclidinyl benzilate (QNB) is a potent, atropine-like glycolic acid ester that blocks acetylcholine muscarinic neurotransmission in the CNS and PNS (6). Halogenated derivatives of QNB are under development as clinical tools to quantify the regional brain distribution of cell-surface muscarinic receptors by single photon ...
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Properties of a quinuclidinyl benzilate binding component in the bulb mite

Comparative Biochemistry and Physiology Part C: Comparative Pharmacology, 1990
Abstract 1. 1. About 95% of the specific binding (defined by atropine) of the muscarinic ACh receptor antagonist [ 3 H]-quinuclidinyl benzilate occurred in the low speed pellet (5500 g , 10 min) of whole bulb mite homogenates and was heat sensitive, linear with tissue concentration and saturable. Rosenthal analysis indicated that [ 3 H]QNB was
Zhiyong Huang, Charles O. Knowles
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Cerebrovascular transport of [125I]quinuclidinyl benzilate, [3H]cyclofoxy, and [14C]iodoantipyrine

American Journal of Physiology-Heart and Circulatory Physiology, 1990
The transport rate constants across rat brain capillaries of a muscarinic acetylcholine receptor antagonist, [125I]quinuclidinyl benzilate (IQNB), an opiate receptor antagonist, [3H]cyclofoxy (CF), and a highly diffusible blood flow indicator, [14C]iodoantipyrine (IAP), were determined by the indicator-diffusion technique and a model that includes a ...
Y, Sawada   +5 more
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The schedule dependent effects of 3-quinuclidinyl benzilate on operant behavior in the rat

Pharmacology Biochemistry and Behavior, 1986
The effects of 3-quinuclidinyl benzilate (QNB) on performance maintained by a fixed-ratio 20 (FR-20) or a differential-reinforcement-of-low-rate 20 sec. (DRL-20) schedule for water reinforcement were studied in rats. Graded doses of QNB (range 0.0125-0.2 mg/kg) were administered IP immediately prior to 30 min test sessions. QNB had a biphasic effect on
W F, Liu, J M, Beaton
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Aging and rat brain muscarinic receptors as measured by quinuclidinyl benzilate binding

Neurochemical Research, 1980
Measurement of cholinergic muscarinic receptor binding in various rat brain areas using the ligand [3H]quinuclidinyl benzilate indicates that receptor binding is decreased in striatum and cerebellum of aged female rats (22 months old) as compared to younger rats (4 months old).
A M, Morin, C G, Wasterlain
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Biphasic effects of 3-quinuclidinyl benzilate on spontaneous motor activity in mice

Psychopharmacology, 1984
Dose-response relationships for onset, duration, and magnitude of 3-quinuclidinyl benzilate (QNB) on spontaneous motor activity (SMA) were studied in mice. QNB was administered SC immediately before 2-h test sessions in dose levels differing by a factor of 0.5 log (range 0.1-10.0 mg/kg).
W F, Liu, N W, Hu, J M, Beaton
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Pharmacologic identification of muscarinic receptors in the pylorus of the cat by binding of [3H]-quinuclidinyl benzilate

Life Sciences, 1980
Muscarinic receptors in the smooth muscle of the cat pylorus (pyloric sphincter) were identified by binding of the ligand (±) [3H]-quinuclidinyl benzilate ([3H]-QNB). Receptor related binding of [3H]-QNB reached steady-state in thirty minutes at 37°C, was saturable, showed pharmacologic specificity and was stereoselective.
T S, Gaginella   +3 more
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