PHRM30002 Lecture Notes - Lecture 8: Analgesic, Hypnotic, Phenobarbital

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Related metabolically and functionally to glu (glutamate) major. Aa nt mediate fast inhibitory and excitatory signalling in the cns. Aa r broadly similar to classical nt r, differ in details of excitatory nt regulation and activation. Multiple receptor signalling systems (ionotropic and metabotropic: unique actions and pharmacology. Therapeutic relevance: sedatives, hypnotics, muscle relaxants, anticonvulsants. Glycine has similar roles in spinal cord. Problem with glu: drugs suppress too much, affects physiological functions. Glutamine/alpha-kg glutamate gaba ssa (tca cycle) Learning and memory (hippocampus), cognition, pain and nociception. Stroke, motor neuron disease, multiple sclerosis, huntington a(cid:374)d pa(cid:396)ki(cid:374)so(cid:374)"s d. Gaba shunt: synthesis, conservation and metabolism of gaba. Astrocyte: responsible for gaba (50%) and glutamate (90%) reuptake communication b/n inhibitory neuron (gaba) and excitatory neuron (glutamate) No receptor on astrocytes: gabaa r ionotropic. Glu r not closely related to those of other nt. Ionotropic (iglurs) nmda or non-nmda (kainite, ampa: nmda: slow, post-synaptic. Binding gaba to gabaa r: receptor activation, cl- entry, hyperpolarisation.

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