Medicinal Chemistry
The pharmacology of all these neuroleptics is extremely complex. Briefly, phenoth- iazines and related drugs have a calming effe ...
It should be emphasized that, whereas neuroleptic control of schizophrenic symptoms has been spectacularly successful since the ...
With prolonged administration, L-DOPA causes undesirable involuntary movements. Moreover, after 4–5 years, Parkinson’s patients ...
In addition to successful dopaminergic-based therapies, antimuscarinic anticholiner- gic agents (see section 4.2.5) are also use ...
system, the hematological system, and the central nervous system. Because of this diverse participation in many physiological pr ...
the past decade, receptor cloning and sequencing has greatly facilitated clarification of this confusing picture. The large numb ...
identified. The 5 - HT 5 familyis a group of receptors that is coupled to neither adenylyl cyclase nor PI-PLC; the family has tw ...
4.5.3.2 Serotonin Reuptake Inhibitors Reuptake through the presynaptic membrane is the major deactivation mechanism for serotoni ...
characterized by muscle rigidity, hyperthermia (fever), myoclonus (brief lightning-like muscle twitches), and rapid changes in t ...
as toad-skin secretion (hence the name; Bufo=toad), bufotenin methyl ether, and a piperazine derivative called quipazine (4.118) ...
5-HT antagonists and is used for the prevention, but not the treatment, of migraine headaches. Ergotamine (4.124), another ergot ...
Because of the widespread importance of serotonin, the development of serotonin antagonists is a continuing area of research end ...
Phenylethylamine, a fragment of LSD, and a number of alkoxyphenylethylamines have been used by various aboriginal societies as h ...
(especially those who both smoke and are receiving the birth control pill), migraine can be a risk factor for stroke. Since migr ...
for the treatment of a severe intractable migraine. Another ergot derivative, methysergide (4.123), is a safer compound for chro ...
4.6.1 Structure, Conformation, and Equilibria of Histamine Protonation has been an important aspect in the design of some histam ...
262 Figure 4.10Top: Ionic and tautomeric equilibria between histamine species and their respective mole percentages. Bottom:4-su ...
NEUROTRANSMITTERS AND THEIR RECEPTORS 263 the blood–brain barrier, central receptors can use only the locally synthesized histam ...
H 2 receptors are localized to the cortex and striatum and are found in neurons, glial cells (astrocytes), and blood vessels. T ...
well as of donating and accepting hydrogen. It produces a higher maximum gastric acid secretion in dogs than does histamine. The ...
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