Functional Groups And Everything Else Flashcards
-OH
Hydroxyl Group (alcohol)
Catechol and pheyl groups
COOH
Carboxyl group acid
Amine Group
NH2
Amino acide
Has both amine group and carboxyl group
COH
Aldehyde
Oxidize of Aldehyde gives COH
Acid COOH
Glycine
Amino acid
Simplist form
Affinity
Likehood that a Ligand can bound to a receptor
Kd and IC50
Measure the affinity either by
Kd dissacosiation constant how much kigand it takes to occupy 50% of receptors
CANNABINOIDS
Anandamide (AN)
2-arachidonoylglycerol (2-AG)
Synthesized from arachinoid acid
PETPTIDES: OPIATES
Endorphins (a, b, g; alpha, beta, gamma)
Enkephalins (Met-enkephalin, Leu-enkephalin)
Dynorphins (dynorphin A, dynorphin B)
Sympathetic
: NE is neurotransmitter. Promotes
energy expenditure, activated by emotion and stress (e.g. increases heart rate, blood pressure, decreases lung secretions)
(Alpha and Beta receptors)
Parasympathetic
ACH is neurotransmitter. Promotes digestion and excretion (e.g., decreases heart rate & blood pressure, stimulates salivation, lung secretions, stomach and intestinal activity, excretion)
(muscarinic receptors)
Potency
At what doses does the drug have its effect? How much of the drug is necessary?? Often measured by ED50. ED50 is inversely related to potency.
EFFICACY:
Effect of the drug on system or organism (not just intrinsic cellular activity), e.g., therapeutic efficacy. Efficacy can vary from drug to drug. Also, it can be expressed as % of subjects showing an effect, or the magnitude of the effect by some direct measure.
Determined by maximal affect
ED50
ED50: effective dose 50; dose that gives 50% maximal effect; measure of POTENCY of the drug
Tolerance:
reduced potency, and sometimes reduced efficacy, with repeated dosing
Sensitization
: increased potency, and sometimes increased efficacy, with repeated dosing
Affects on the dose/response curve
Competitive Antagonists: Competitive antagonists produce a parallel shift to the right in the dose/response curve for agonists
Non-competitive antagonists: shift agonist dose response curve, and reduce maximum response
ALLOSTERIC MODULATOR
binds to a different site on the receptor (called the allosteric site), modulates affinity of the receptor for its transmitter (e.g. benzodiazepines such as Valium are positive allosteric modulators of the GABAA receptor; facilitate the inhibitory actions of GABA, enhance affinity for GABA)
reversible antagonist
binds non-covalently to the receptor, binding is very transient, and therefore it can be displaced by a ligand that binds to the same receptor.
INVERSE AGONIST:
binds to receptor, stimulates intrinsic activity opposite of neurotransmitter
nigrostriatal
(substantia nigra pars compacta (SNc) to caudate/putamen (CPU, neostriatum, “striatum”); involved in aspects of learning, compulsive behavior, habit formation and motor control; degenerates in Parkinson’s Disease, mediates Parkinsonian side effects of antipsychotics
mesolimbic
(VTA to nucleus accumbens); involved in motivation, behavioral activation, effort expenditure, learning, aspects of drug abuse, depression, schizophrenia
mesocortical
(VTA to prefrontal and cingulate cortex); involved in schizophrenia, depression, ADHD, stress, learning, decision making
intrinsic striatal neurons
(start and end within the CPU/ striatum); site of ACH/DA interaction in Parkinsonism
basal forebrain system
(originate in or near septum, also basal nucleus, projects to neocortex and hippocampus) degenerates in Alzheimer’s disease, involved in cognition
ventral bundle
(brainstem to hypothalamus); involved in food intake, stress
For NE
dorsal bundle
(locus coeruleus projects to neocortex and hippocampus); involved in learning, attention, ADHD, stress, depression
raphe system
(midbrain/pons projects to hypothalamus, striatum, cortex, hippocampus); involved in depression, anxiety, stress, drug abuse, motor control, learning
