Medicinal Chemistry
parasympathetic terminals involved in gastrointestinal and ureteral peristalsis, glandular secretion, pupillary constriction, pe ...
where Ca2+-mediated vesicle fusion occurs. Historically, botulinum toxin was of interest because of its role in botulism food po ...
Torpedo electric organ. Compared to normal concentration standards, this yield is exceptionally high. 4.2.2.2 Physicochemical Pr ...
Various pharmacologic and molecular biology studies have identified at least two distinct types of nicotinic cholinergic recepto ...
effects, or both; and (2) by binding of the indirect agonists, which are drugs that inhibit the hydrolysis of ACh by AChE, thus ...
Ammonium Group.The ammonium group of ACh can be replaced by other “-onium” compounds (phosphonium, arsonium, or sulfonium), but ...
4.2.4.2 Cholinergic Agonists: Mode of Binding of Acetylcholine The acetylcholine molecule is highly flexible, and its preferred ...
(section 4.6.5). Atropine has been used to treat urinary urgency associated with bladder inflammation; oxybutynin (4.13), anothe ...
These tropine derivatives are esters of tertiary bases with a bulky acid component (atropic acid, mandelic acid). In general, a ...
4.2.5.2 Cholinergic Antagonists: Neuromuscular Blocking Agents Neuromuscular blocking agents are widely used in surgery. They ar ...
the same response as does ACh—a brief contraction of the muscle—which, however, is followed by a prolonged period of transmissio ...
disease is associated with brain atrophy and loss of the outer gray matter of the cerebral cortex. At the cellular level, the hi ...
4.3 NOREPINEPHRINE AND THE ADRENERGIC RECEPTORS 4.3.1 The Adrenergic Neuronal System Norepinephrine is another important neurotr ...
is therefore the logical point for the inhibition of NE synthesis. DOPA decarboxylase acts on all aromatic amino acids and requi ...
(embryologically, the medulla is a modified ganglion and therefore uses ACh as a transmitter). This allows the inflow of Ca^2 +, ...
aliphatic amines. MAO is, in itself, an important target in drug design and is discussed separately in chapter 8 since it repres ...
The other enzyme in catecholamine catabolism is catecholamine O-methyltransferase (COMT), a cytoplasmic enzyme that uses S-adeno ...
norepinephrine>isoproterenol. The βreceptors are usually inhibitory on smooth muscle but stimulate the myocardium. Their drug ...
respectively. This structure for the βadrenergic receptor is similar to other G-protein- linked receptors whose cDNAs have been ...
gene was first described in the Pima Indians, a population with a high incidence of obesity. In the human receptor, this substit ...
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