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The Heart of Matter
 Among the many relevant phenol
derivatives, the catechol neurotransmitters are
some of the most valuable and interesting.
 The nervous system runs on a series of physical and
chemical reactions. Signals are carried from one nerve cell to
another by simple chemical molecules known as
neurotransmitters. Epinephrine (adrenalin), norepinephrine,
dopamine, and acetylcholine are but four of the more than 20
known neurotransmitters.

 The first three substances are also called catecholamines because they are
similar to catechol, or o-hydroxyphenol
 The sympathetic nervous system (SNS)
and the parasympathetic nervous system
(PNS) stimulate almost every organ in the
body in a complementary fashion. The PNS
supplies the stimulation for normal
physiological functions, while the SNS
provides the necessary arousal for survival
in the “cold, cruel world”.
 The PNS is responsible for contraction of
the pupils of the eyes, normal pulse and
blood pressure, constriction of the bronchi,
digestive enzyme-containing secretions in
the mouth, and increased gastrointestinal
activity. The SNS in an effort to make the
body alert and ready to respond to any
outside threat, causes dilation of the pupils,
increased pulse and blood pressure, and
relaxation of the bronchi, dry mouth, and
decreased gastrointestinal motility.
 The prime neurotransmitter in the SNS is
norepinephrine. It is synthesized in an SNS
nerve cell and, in response to a nerve impulse,
is secreted into the space between two nerve
cells, called the synapse. The neurotransmitter
travels to the other side of the synapse and
combines with a protein known as a receptor
on the surface of the next nerve cell. This
triggers the nerve impulse in that cell.
 Molecules that are similar in structure to a
natural neurotransmitter can either stimulate a
nerve cell just like the natural chemical
(agonists) or bind to the receptor without
stimulation and block the access of the normal
neurotransmitter (antagonists).

 Agonist-receptor complex stimulates nerve transmission.

 Antagonist-receptor complex causes no nerve
stimulation and blocks normal stimulation.
 Amphetamines and decongestants are
examples of SNS agonists. Although these
drugs may be used for certain specific effects,
such as in dieting and for nasal congestion,
respectively, it is important to remember that
they are similar to the natural
neurotransmitters that generally affect the SNS
and also the central nervous system, which is
far too complex to discuss in this space. Thus
the warnings on the containers for many over-
the-counter medications should be heeded,
especially if the consumer has a preexisting
condition such as high blood pressure,
diabetes, or glaucoma.
 Another aspect of drug use involves the
design of neurotransmitter antagonists, as in
the treatment of heart disease. Many types of
neurotransmitter receptors exist, some of
which are concentrated in specific tissues, such
as heart tissue (β1-receptors) and bronchial
tissue (β2-receptors). Β1-blockers have been
designed to antagonize the nerve signals to the
heart without having an effect of equal
intensity on breathing.
 Conversely, a drug that is specific for β2-
receptors could be used as an agonist to
relieve asthma without worsening an existing
cardiac condition.

 The treatment of disease had reached a

molecular level, leading to more potent and
specific drugs with the possibility of living a
longer and more enjoyable life.
 Β-blockers:

 Β2-receptor agonists: