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Digitale Medien

3H-Domperidone: A selective ligand for dopamine receptors (1979)

Baudry, M. ; Martres, M. P. ; Schwartz, J. C.

Springer

Naunyn-Schmiedeberg's archives of pharmacology 308 (1979), S. 231-237

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Details

ISSN: 1432-1912

Schlagwort(e): 3H-Domperidone ; Dopamine receptors

Quelle: Springer Online Journal Archives 1860-2000

Thema: Medizin

Notizen: Summary 3H-Domperidone, a potent antagonist of dopamine but less lipophilic than neuroleptic drugs, was studied as a potential ligand for cerebral dopamine receptors. It labeled with high affinity an apparently homogeneous population of non-interacting sites in a particulate fraction of mouse striatum. Association occurred rapidly and dissociation was relatively slow (t1/2≃4min); this allowed extensive washing of membranes which reduced the non-specific binding to values as low as 5% of the total binding. Consistent Kd values of 0.7 nM were obtained by analysing by various methods either the kinetics of binding or the saturation of binding sites at equilibrium. The relative potencies of various dopamine receptor agonists or antagonists to inhibit 3H-domperidone binding, paralleled their pharmacological activity. On the other hand, a variety of non-dopaminergic agents failed to inhibit 3H-domperidone binding. The findings indicate that striatal dopamine receptors are selectively labeled by this 3H-ligand. In various non-striatal regions of mouse brain the saturable binding of 3H-domperidone was almost entirely inhibited by apomorphine indicating its selectivity for dopamine receptors in spite of the low density of the latter. This was not the case for the binding of 3H-spiperone, evaluated on the same preparations, indicating that 3H-domperidone probably represents the most selective ligand presently available.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF00501387

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Digitale Medien

The functional relationship scan in tandem mass spectrometry (1988)

Vincenti, M. ; Schwartz, J. C. ; Cooks, R. G. ; [weitere]

Chichester : Wiley-Blackwell

Biological Mass Spectrometry 23 (1988), S. 579-584

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ISSN: 0030-493X

Schlagwort(e): Chemistry ; Analytical Chemistry and Spectroscopy

Quelle: Wiley InterScience Backfile Collection 1832-2000

Thema: Chemie und Pharmazie

Notizen: A type of tandem mass spectrometric scan is described in which m1 +, m2 + and m3, defined in terms of the process m1 + → m2 + + m3, are all varied while maintaining some prescribed relationship between them. The scan can be viewed as a variant upon the neutral loss scan in which the constant mass difference between parent and daughter ion masses is replaced by some other functional relationship. Specific examples of this scan are provided in two simple applications: (i) symmetrical proton-bound dimers are recognized using the functional scan m2 = (m1 + 1)/2; and (ii) symmetrical Diels-Alder adducts comprised of diene and dienophile of equal masses are recognized in mixtures using the scan function m2 = (1/2)m1.

Zusätzliches Material: 4 Ill.