PHRM 211 Lecture Notes - Lecture 5: Adenylyl Cyclase, Gaba Receptor, Gaba Transporter

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14 Apr 2020
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Med chem of neuromodulator drugs (part 1) Most excitatory neurotransmitter in the human cns. Estimated to be involved in 70% of fast excitatory synapses. Cotransported by excitatory amino acid transporters (eaats) with 3 na+ & h+ for k+ Three major ionotropic glutamate receptors are distinguished pharmacologically increase na+ influx (also ca2+ for nmda) & k+ efflux. 80 mv reduced to -90 mv resting potential) Most inhibitory neurotransmitter in the human cns (used by 1/3 of all cns synapses) Gaba a receptors are ionotropic pentameric cl- channel hyperpolarize cells (-50 to. Gaba b receptors are metabotropic heterodimeric gpcrs negatively regulate adenylyl cyclase & voltage-gated ca2+ channels, positively regulate inwardly rectifying k+ channels; receptor activation leads to cell hyperpolarization. Drugs that oppose glutamate activity or enhance gaba activity contribute to cell hyperpolarization. Targets not only include receptors , but also enzymes (e. g. gaba metabolism) and transporters (e. g. synaptic gaba reuptake) Does not bind to gaba a or gaba b receptors.

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