PCOL2605 Lecture Notes - Lecture 29: Nmda Receptor Antagonist, Ampa Receptor, Metabotropic Receptor

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2 main types of synapses: neuromuscular junction, neuron-neuron synapse. Pgp pushes the molecule back out of the brain. Biggest target for drugs in the brain is synapses. Amino acid neurotransmitters: gluta(cid:373)ate: (cid:373)ai(cid:374) e(cid:454)(cid:272)itator(cid:455) amino acid neurotransmitter, gaba: (cid:373)ai(cid:374) i(cid:374)hi(cid:271)itor(cid:455) a(cid:373)i(cid:374)o a(cid:272)id (cid:374)eurotra(cid:374)s(cid:373)itter, gl(cid:455)(cid:272)i(cid:374)e: se(cid:272)o(cid:374)dar(cid:455) i(cid:374)hi(cid:271)itor(cid:455) a(cid:373)i(cid:374)o a(cid:272)id (cid:374)eurotra(cid:374)s(cid:373)itter. Glutamate opens an ion channels and a metabotropic receptor (gaba) When you effect it you effect everything: what is a (cid:373)ore su(cid:271)tle (cid:449)a(cid:455) of alteri(cid:374)g ampa re(cid:272)eptor activity, what is a(cid:374) allosteri(cid:272) (cid:373)odulator, allosteric modulators are promising. Cyclothiazide, piracetam and cx-516 subtly increase ampa respo(cid:374)ses to ampa. Possi(cid:271)le (cid:272)og(cid:374)itio(cid:374) e(cid:374)ha(cid:374)(cid:272)ers, adhd, parki(cid:374)so(cid:374)(cid:859)s, depressio(cid:374: per(cid:373)apa(cid:374)el: (cid:374)o(cid:374)-competitive antagonist used for epilepsy, kai(cid:374)ate- possibly better as less widely distributed glutamate. But many agonists cause hallucinations and other mental disturbances. Memantine (axura and akatinol) low affinity, non-competitive antagonist used for alzheimers disease. Does not stop progression but reduces some symptoms for some.

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