G examples of drugs affecting dopaminergic

This preview shows page 14 - 19 out of 29 pages.

g.Examples of drugs affecting dopaminergic neurotransmission:i.Antiparkinsonian drugs1.Levodopa and Selegilininhibits MAO-B2.Entacaponinhibits COMTii.Antipsychotic drugs1.Dopamine receptors antagonistiii.Antidepressantsinhibits MAO (degrade dopamine)iv.Cocaineblocks dopamine transporter DAT1.Addictioncomes from the blockade ofDATh.Receptors for Dopamine are all GPCRSi.D11.D1 and D5stimulate AC2.Cerebral cortex and limbic systemii.D2iii.D2, D3, and D4inhibit ACi.Norepinephrine:i.Most cell bodies in CNS are in locus coeruleus in ponsii.Important forSleep, arousal, attentions and learning.iii.Plays a rolein depression and anxiety1.GPCRs:a.Alpha 1b.Alpha 2
j.Serotonin: 5-HTi.Cell bodies are in the Raphe Nucleus (brain stem)ii.Role in depression and emesisiii.Serotonin transporter(SERT) site of action of SSRIs
iv.v.Serotonin receptors:1.7 main types2.ALLGPCRsexcept5-HT3vi.Main 5-HT receptors:1.5-HT1a.Most widespread2.5-HT2a.Targeted by atypical antipsychoticsb.Found in amydala ,cerebral cortex, hippocampus,basal ganglia3.5-HT3a.Targeted by antiemetic’s (ondansetron)b.Low 5HT3i.Limbic system, hippocampus, cerebral cortexc.High 5-HT3i.Area postremaii.Tractus solitariusk. Acetylcholine:1.Important for cognition2.Therapeutic target in Alzheimer’s and Parkinson’s disease3.Bind to Muscarinic receptors
4.Bind to nicotinic receptors
5.Both are highly expressed in thecerebral cortexl.Histamine:
1.In CNS produced by hypothalamus2.GPCRS3.Central H1 receptors responsible for side effects of oldgeneration antihistaminesclozapinem. Endocannabinoids:i.CB1 and CB2 receptorsGPCRii.CB2peripheral onlyiii.Two main agonist1.Anandamide2.1-archindonoylglyceroliv.Plays a role inreward, pain and movementv.CB1 agonists are antiemetic’s and stimulate appetite.8.What types of cells are in the CNS?
Day 3:1.List main antiparkinsonian drugs?a.Carbidopab.Levodopac.Entacapone, Tolcaponed.Selegiline, Rasagilinee.Bromocriptine (ergot derivative)f.Pramipexole, Ropinirole, Rotigotine (Non-ergot derivative)2.Describe mechanisms of action of these drugs and how it relates to disease pathology ?
a.b.Metabolism of Dopamine
i.c.How the drugs react to the pathwayi.Carbidopaii.Prevent peripheral breakdown of levodopaiii.DDC inhibitorsiv.Levodopa1.Converted to dopamine within the braind.Entacapone, Tolcaponei.COMT inhibitorsii.Prevent peripheral breakdown of levodopae.Selegiline, Rasagilinei.MAO-B inhibitorsii.Prevent further breakdown of dopamineiii.Block degradation of dopaminef.Bromocriptine, Pramipexole (Mirapex), Ropinirole (Requip),Rotigotine (Neupro)i.Dopamine Agonistii.Post-synapticmimicryof naturallyoccurring dopamine.

Upload your study docs or become a

Course Hero member to access this document

Upload your study docs or become a

Course Hero member to access this document

End of preview. Want to read all 29 pages?

Upload your study docs or become a

Course Hero member to access this document

Term
Fall
Professor
BOWMAN
Tags
levodopa

  • Left Quote Icon

    Student Picture

  • Left Quote Icon

    Student Picture

  • Left Quote Icon

    Student Picture