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Muscarinic acetylcholine receptors in the pig  

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MUSCARINIC ACETYLCHOLINE RECEPTORS IN THE PIG ABSTRACT 1. Muscarinic receptors in porcine caudate nucleus and urinary detrusor smooth muscle were examined using the non-selective muscarinic receptor antagonist radioligand [3H]-QNB. Muscarinic receptor-evoked contractile responses were investigated using strips of porcine urinary detrusor. 2. On comparing pKi values obtained with values and rank orders of affinity relating to human cloned receptors, it was concluded that M1 receptors are found in the caudate nucleus. M2 and M3 receptors are found in the bladder detrusor muscle. Using information gained from this experiment, use of antimuscarinics in the therapy of urinary incontinence was discussed with emphasis on Oxybutynin and its side effects due to non selective effects on muscarinic receptors in the central nervous system. Abbreviations: MAChR, muscarinic acetylcholine receptor; QNB, quinuclidinylbenzilate; INTRODUCTION Receptor physiology Muscarinic receptors are a class of acetylcholine receptors. They are G-protein coupled (7-transmambrane spanning receptors) coupled to intracellular effector systems through a G protein. They have various biochemical...

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