Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C1323099 (sympathomimetic)
 2,957 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The conformationally restricted cis and trans isomer of substituted cyclobutanes were examined for their ability to inhibit 3H-norepinephrine and 3H-dopamine accumulation by synaptosomes prepared from the cortex and corpus striatum, respectively. The drugs were more effective in preventing the accumulation of 3H-norepinephrine by cortical synaptosomes than 3H-dopamine by striatal synaptosomes. However, in the synaptosomes isolated from both regions, the trans isomers were more potent inhibitors of accumulation than the cis isomers. The greatest stereoselectivity was exhibited by the isomers of 2-amino-1-phenylcyclobutanol. The accumulation of 3H-norepinephrine by cortical synaptosomes and the accumulation of 3H-dopamine by striatal synaptosomes were inhibited 50% by concentrations of the trans isomer of 7.4 X 10(-6) M and 1.7 X 10(-4) M, respectively. The cis isomer was inactive. In separate experiments, the releasing capabilities of the restricted analogs were determined by superfusing cortical and striatal synaptosomes labelled in vitro with 3H-catecholamines. The trans and cis isomers elicited a trivial release of 3H-norepinephrine and 3H-dopamine from cortical and striatal synaptosomes, respectively. The results indicate that the decreased synaptosomal accumulation of 3H-catecholamines caused by the analogs was due mainly to inhibition of uptake. The influence of dihydral angle between phenyl--NH2 on the inhibition of uptake is discussed. It is concluded that the anti conformation of sympathomimetic amines is the preferred conformation at the noradrenergic amine pump.
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PMID:Inhibition of synaptosomal uptake of norepinephrine and dopamine by conformationally restricted sympathomimetic amines. 72 Mar 87

1. In the driven rabbit left atrium alpha-adrenoceptors mediate the inotropic effect of phenylephrine and the prolongation of functional refractory period by sympathomimetic amines.2. These receptors are highly sensitive to blockade by phentolamine and phenoxybenzamine.3. Prolongation of functional refractory period is greater with the secondary amines, phenylephrine, adrenaline and epinine, than with the primary amines, norphenylephrine, noradrenaline and dopamine.
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PMID:Characterization of -adrenoceptors in the myocardium. 414 62

A stereospecific synthesis of endo-2-aminobenzornorbornene is described. Its sympathomimetic activities and those of its N-methyl derivative were compared with the equivalent exo-isomers using the isolated rat anococcygeus muscle and the anaesthetized rat blood pressure preparations. On the anococcygeus muscle preparation the endo- and exo-isomers of the primary amines had similar indirectly acting sympathomimetic activities. In contrast the exo-N-methyl derivative was a far more potent sympathometic in vitro than the endo-N-methyl isomer. In the anaesthetized rat the exo- and endo-isomers of 2-aminobenzonorbornene and their N-methyl derivatives all had similar pressor activities, though the successive injections of the two exo-derivatives suggested an additional alpha-adrenoceptor blocking activity. The actions of these rigid sympathomimetics are compared with those of the flexible amphetamine structure.
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PMID:Sympathomimetic effects of exo- and endo-isomers of 2-aminobenzonorbornene in vitro and in vivo. 610 48

A sensitive and rapid method for the gas chromatographic (with electron-capture detection) confirmation of derivable sympathomimetic amines is described. Extractive derivatization with pentafluorobenzoyl chloride is performed on 2-ml urine or plasma samples. Especially for primary amines, the method appears to be very sensitive. Mass spectral data allowed confirmation of the monobenzoylation of all congeners.
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PMID:Pentafluorobenzoyl derivatives of doping agents. I. Extractive benzoylation and gas chromatography with electron-capture detection of primary and secondary amines. 685 43

Derivatives of some primary amines and their N-benzyl derivatives containing a 4-cyclohexylphenyl or a 4-phenylcyclohexyl group were prepared. Pharmacological study showed clear analgesic activity in the phenylquinone test which was more accentuated for the 4-phenylcyclohexyl derivatives. All the compounds proved devoid of sympathomimetic activity on the cardiovascular system and without anorexic effect. Some of the compounds showed some antireserpine activity.
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PMID:[A new cyclohexylphenyl and cyclohexylphenylamine. Synthesis and pharmacological activity]. 745 27

Interactions between some novel and potent monoamine oxidase inhibitors (MAOIs), acetylenic analogues of tryptamine, and rat liver microsomal cytochrome P450 (P450) as evidenced by visible spectra analysis were analysed. Compounds with a secondary aliphatic amine moiety throughout induced type II difference spectra and exhibited the highest affinity for P450, whereas tertiary amines induced type I spectral changes and showed diminished affinity. P450 dependent aniline hydroxylase activity was inhibited by all compounds in an irreversible time-dependent manner. Only tertiary aliphatic amines constituted the substrate for P450-dependent N-demethylase activity, with comparable kinetic parameters. The N-demethylated metabolites were identified by thin-layer chromatography and mass-spectrometric analyses. These findings describe the role of P450-dependent microsomal mono-oxygenase systems in the metabolism of some MAOI acetylenic tryptamine derivatives and the possible hepatic contribution to adverse interactions between MAOIs, endobiotics and sympathomimetic compounds.
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PMID:Interactions of monoamine oxidase inhibitors, N-acetylenic analogues of tryptamine, with rat liver microsomal cytochrome P450. 808 7

Pediatric incontinence is a bothersome symptom for children and their parents. It can have a profound influence on a child's social and psychologic development and well-being. It is important to understand the different disorders that result in incontinence and also to understand the neural influences and development on urinary control. Urinary leakage can be a functional or organic disorder, with many possible etiologies. The most common group of pediatric patients with incontinence are those with overactive bladder disorder. Pharmacologic therapy centers on the blockage of muscarinic receptors by the tertiary amines such as oxybutynin, tolterodine, trospium chloride, and propiverine. Although most novel anticholinergic medications are effective and well tolerated in children, in our experience oxybutynin extended release provides superior relief for urge urinary incontinence in children. Other agents such as alpha-adrenoceptor antagonists have been used with success to improve bladder empyting and decrease outlet resistance. Night-time voiding disorders such as primary monosymptomatic nocturnal enuresis tend to be symptomatically treated. One of the mainstays of pharmacotherapy is desmopressin, an analog to antidiuretic hormone, which decreases night-time urine production. Tricyclic antidepressants such as imipramine have also been used successfully through a combined mechanism of action believed to be the result of anticholinergic, antispasmodic, and sympathomimetic effects. Often the successful treatment of constipation also treats urinary incontinence or at least the symptoms of urinary leakage are improved. The new non-absorbable, tasteless, and odorless PEG-3350 (polyethylene glycol 3350) powder has quickly become a mainstay of the pharmacologic treatment for constipation because of its ease of preparation and favorable adverse effect profile. A better understanding of the physiologic control, cellular interactions, and second messenger signal transduction pathways has led to the development of many new potential target sites for pharmacologic intervention. The advancement of new uroselective muscarinic antagonists is currently under investigation for agents such as darifenacin and temiverine, which have the potential to improve efficacy without increasing unwanted adverse effects. New pharmacologic delivery systems are also being developed ranging from intravesical to transdermal applications to change biodistribution and improve selectivity. Incontinence is a significant problem for children, their parents, and their physicians. The changing and advancing field of pharmacotherapy has made big strides for symptom control in this patient population.
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PMID:Contemporary and emerging drug treatments for urinary incontinence in children. 1597 61