Lecture-11-2011-Bi-CNS150

Lecture-11-2011-Bi-CNS150 - enzyme inhibitors...

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Bi / CNS 150 Lecture 11 Wednesday, October 19, 2011 Recreational drugs Henry Lester This material is scattered throughout Kandel; see Nestler enzyme inhibitors neurotransmitter transport inhibitors
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2 Disclaimer 1. Do not alter your pattern of prescription drug compliance as a result of this course. 2. Consult a medical professional for further guidance about prescription drugs. H. A. L. is not aware of all trends in current medical practice, is not a physician, and cannot prescribe.
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3 NH 2 CH 3 amphetamine N N CH 3 C N C 2 H 5 C 2 H 5 O LSD H 3 C H 2 C OH ethanol N CH 3 N nicotine N O HO HO CH 3 morphine N phencyclidine O H 3 C H 3 C CH 3 OH C 5 H 11 tetrahydrocannabinol N OC O C O CH 3 O H 3 C cocaine N N N N O O H 3 C CH 3 CH 3 caffeine Recreational drugs Addictive drugs
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4 Coca Harvest in Bolivia, ca. 1950
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5 cocaine in the test tube H + N OC O C O CH 3 O H 3 C cocaine base: directly extracted from the plant with organic solvents treatment with HCl + HN OC O C O CH 3 O H 3 C Cl - cocaine hydrochloride: a salt, readily soluble treatment with base: ammonia or Na bicarbonate, then heat to drive off HCl “crack” cocaine
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6 H + blood lungs, nose, stomach N OC O C O CH 3 O H 3 C + HN OC O C O CH 3 O H 3 C H + N OC O C O CH 3 O H 3 C + HN OC O C O CH 3 O H 3 C cocaine base (crack) cocaine in the body cocaine hydrochloride Cl - South American Indians use Ca(OH) 2 from limestone to shift this equilibrium Lipid barrier, e. g. membrane(s)
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7 neurotransmitter transporters ligand-activated channels GPCRs G protein-activated channels N C LSD morphine-heroin tetrahydrocannabinol amphetamine cocaine phencyclidine nicotine ?alcohol? caffeine* (*= intracellular target) enzymes Targets for Recreational Drugs α
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8 Na + -coupled cell membrane neurotransmitter transporters: Antidepressants (“SSRIs” = serotonin-selective reuptake inhibitors): Prozac, Zoloft, Paxil, Celexa, Luvox Drugs of abuse: MDMA Attention-deficit disorder medications: Ritalin, Dexedrine, Adderall Drugs of abuse: cocaine amphetamine Na + -coupled cell membrane serotonin transporter Na + -coupled cell membrane dopamine transporter N H HO NH 3 + HO HO H 2 C C H 2 NH 3 + cytosol outside major targets for drugs of therapy and abuse Presynaptic terminals From Previous Lectures Trademarks:
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Lecture-11-2011-Bi-CNS150 - enzyme inhibitors...

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