[PHAR 435] - Midterm Exam Guide - Comprehensive Notes for the exam (16 pages long!)

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The g-protein muscarinic ach receptors constitute a family with 5 subtypes (m1-m5) M1, m3, and m5 are excitatory they are coupled to gq/g11 and activate plc. Generates ip3 and dag = ca2+ release. M2 and m4 are inhibitory they inhibit ac via gi/go = camp production. Choline is attached to acetylcoa in the body by choline acetyltransferase (reversed by ach esterase) Drug targets = ach esterase and choline esterstransferase. Analogues display significant selectivity toward m-ach receptor vs. n-ach ion channel. Amide resonance increases stability against the ach esterase. Larger ester motifs result in loss of activity (but the binding is still in tact therefore, these compounds will act as antagonists ex. atropine) The overall size of the molecule cannot be varied greatly. The n to ester group distance is important. The ethylene linker cannot be extended (but substituents can be added) 2 of the n-substituents must correspond to me (?)

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