Key Concepts
1. Many substances have been identified as
neurotransmitters according to formal criteria. Many more putative transmitters
are being evaluated, so the total number of confirmed transmitters is likely
to continue to grow.
2. Each step in synaptic transmission, from
axonal transport to postsynaptic effects, is a potential target for neuropharmacological
compounds.
3. The search for new drugs and the characterization
of new types of receptors occur in parallel. Sometimes a brain receptor
for a particular exogenous drug is discovered; the existence of such a
receptor implies that the brain makes an endogenous ligand for that receptor.
4. Although drugs frequently have higher affinity
for a particular type of receptor than for other types, the “tuning” of
drugs tends to be somewhat nonspecific. Most drugs, if present in the body
in sufficiently high concentration, will bind to many different types of
receptors.
5. Drugs may affect many different aspects
of presynaptic function, such as alteration in transmitter synthesis, alteration
in transmitter storage, alteration in transmitter release, alteration in
autoreceptor function, blockade of reuptake, and inhibition of breakdown
enzymes.
6. Drugs may affect many different aspects
of postsynaptic function, including activation of postsynaptic receptors,
blockade of postsynaptic receptors, alteration in second messenger activity,
alteration in gene expression, and up- and down-regulation of postsynaptic
receptor density.
7. Repeated use of some drugs causes the development
of tolerance: Repeated doses of the same size have less and less effect.
8. Repeated use of some drugs causes the development
of sensitization: Repeated doses of the same size have greater and greater
effect.
9. Endogenous opiates such as morphine are
powerful analgesics and have considerable abuse potential. Several different
types of opiate receptors have now been identified, along with a number
of endogenous opiate peptides.
10. The existence of cannabinoid receptors
in the brain, through which THC has its effects, implies the existence
of an endogenous ligand, which may be anandamide.
11. In some cases stimulant drugs act by mimicking
the effects of a neurotransmitter; other stimulants act by directly or
indirectly altering the concentration of neurotransmitter in the synapse;
still others act by altering the actions of neuromodulators such as adenosine.
12. Hallucinogenic drugs alter sensory perceptions
rather than provoking true hallucinations. Some hallucinogens act by interacting
with serotonin receptors, but much remains unknown about the physiological
bases of the effects of these drugs.
13. Chronic alcohol abuse alters both the
function and structure of the brain. Happily, these effects are largely
reversible following cessation of the use of alcohol.
14. Several models of drug abuse have been
proposed, none of which explains all of the phenomena associated with dependency.
The positive reward model has received strong support from drug self-administration
studies.
15. Animal models of drug abuse have been
successfully developed because animals will frequently choose to ingest
psychoactive substances and respond to those substances in ways that are
similar to human responses.
16. Recent advances in our understanding of
the neurophysiological bases of drug abuses have led to proposals of several
pharmacological interventions for the treatment of substance-related disorders.