The molecular structure of adrenergic and dopaminergic substances

Giesecke, Johan; Hebert, Hans

doi:10.1017/s003358350000545x

Cited by 16 publications

(4 citation statements)

References 127 publications

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“…The conformations of adrenergic and dopaminergic drugs have been reviewed recently by Duax (1979), Giesecke (1979) and Hebert (1979). The conformations are defined by two torsion angles r I and r 2 as in Fig.…”

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confidence: 99%

(R,R)-Labetalol hydrochloride: determination of the absolute configuration of the high-melting polymorph, C19H25N2O3+.Cl−

Murray‐Rust¹,

Murray‐Rust²,

Hartley³

et al. 1984

Acta Crystallogr C Cryst Struct Commun

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confidence: 99%

(R,R)-Labetalol hydrochloride: determination of the absolute configuration of the high-melting polymorph, C19H25N2O3+.Cl−

Murray‐Rust¹,

Murray‐Rust²,

Hartley³

et al. 1984

Acta Crystallogr C Cryst Struct Commun

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“…The binding techniques have several limitations: exact molecular events in the very interaction 1) The techniques give no direct information between drug and receptor are at present unabout the physiological response to receptor known, though some speculative models have stimulation. This fact is especially true when been proposed (32). The structure-activity relaantagonists are used in the study of the re-tionships for various adrenergic agents have receptors.…”

Section: T 1 •mentioning

confidence: 99%

“…The structure-activity relaantagonists are used in the study of the re-tionships for various adrenergic agents have receptors. The antagonists have been more wide-cendy been reviewed (32). ly used because of their higher specific radioThe molecular nature of the P receptor and activity, their greater stability and lesser non-especially its relationship to the enzyme, adenyspecific binding (58).…”

Section: T 1 •mentioning

confidence: 99%

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Adrenoceptors: Molecular Nature and Role in Atopic Diseases

Djurup

1981

Allergy

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Since Szentivanyi proposed the idea that asthma and other atopic ditseases are due to a P adrenergic defect there has been much interest in the role of the adrenergic receptors in allergy. The radioactive ligand binding techniques developed within the last few years have greatly increased our knowledge concerning the molecular nature of the adrenoceptors and the events following receptor sdmulation. The adrenoceptors have shown to be very dynamic structures. Their number and affinity may be altered due to various physiological and pharmacological stimuli. Their role in the pathogenesis of atopic diseases has not been definitely settled, but there seem to be a true beta adrenergic hyporesponsiveness and alpha hyperresponsiveness in asthma. This article briefly describes the radioligand binding technique and summarizes our present knowledge of the nature of the alpha and beta adrenoceptors and their possible role in atopic diseases.Key words: adrenergic receptors; atopy; asthma. Accepted fcyr publication 11 January 1981, , , rr 1 , ^^ 01 receptor is defmed as a receptor for Functional subclassification of the adrenoceptorswhich epmephrme is a more potent stimulator It has been known since the beginning of the (agonist) than norepinephrine which again is century that the sympathomimetic amines have more potent than isoproterenol. The potency both excitatory and inhibitory effects in the of the amines was examined in intact animals organism. Early investigators proposed the or isolated organ preparations. In contrast, the existence of two fundamental types of mediator P receptor is defined as a receptor for which substances: an excitatory sympathin E and an isoproterenol is a more potent agonist than inhibitory sympathin I (1). As no amine which epinephrine which again is more potent than fulfilled the requirements for either sympathin norepinephrine. The development of relatively E or I could be found, the idea of two different selective a and |3 antagonists has further conreceptor types emerged. On the basis of the firmed the pharmacological usefulness of the a relative potency of six adrenergic amines on and P receptor concept. Table 1 summarizes various biological (mainly haemodynamic) pa-the major pharmacological characteristics of rameters, Ahlquist (1) defined two different the a and the j3 receptor. receptors: an a receptor which mediates most In 1967, Lands (55) showed that there is of the adrenergic amines' excitatory functions marked similarity between the relative poten-(vasoconstriction, pupil dilation, uterine con-cies of sympathomimetic amines on lipolysis traction) and a few inhibitory (intestinal relax-and cardiac stimulation on the one hand and ation), and a P receptor which mediates most of on bronchodilation and vasodepression on the the inhibitory functions (vasodilation, broncho-other. Furthermore, a potent lipolytic and cardilation, uterine relaxation) and a few excita-diac stimulating amine is a poor bronchodilator tory (cardiac inotropy and chronotropy).and vasodepressor. Therefore, Lands s...

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Therapeutic and Diagnostic Agents for Parkinson's Disease

Neumeyer

Baldessarini

Booth³

2003

Burger's Medicinal Chemistry and Drug Discovery

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This chapter considers the biology and medical chemistry‐based treatment of Parkinson's disease, the second most common of the major neurodegenerative neuropsychiatric disorders. It surveys basic clinical features, neuropathology, and etiological theories based on genetics, maturational and oxidative‐metabolic degenerative processes, and environmental neurotoxins including MPTP. Treatments reviewed include L ‐dopa as a replacement therapy, direct dopaminergic agonists and their structure‐activity relationships, and agents that potentiate dopamine by preventing the metabolism of dopa or dopamine by peripheral aromatic amino acid decarboxylase, catechol‐ O ‐methyltransferase, or monoamineoxidase. Drugs acting on nondopaminergic systems considered include anticholinergic, adenosine agonist, glutamate antagonist, and serotonin agonist agents. Agents useful for the diagnosis of Parkinson's disease and monitoring progression of the disease include radioactive dopa and dopamine transporter labeling agents for use in brain imaging. Finally, future directions of efforts to improve the treatment of Parkinson's disease are considered, with an emphasis on the continued central importance of medicinal chemistry.

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The molecular structure of adrenergic and dopaminergic substances

Cited by 16 publications

References 127 publications

(R,R)-Labetalol hydrochloride: determination of the absolute configuration of the high-melting polymorph, C19H25N2O3+.Cl−

(R,R)-Labetalol hydrochloride: determination of the absolute configuration of the high-melting polymorph, C19H25N2O3+.Cl−

Adrenoceptors: Molecular Nature and Role in Atopic Diseases

Therapeutic and Diagnostic Agents for Parkinson's Disease

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