Dihydroergotamine binding to rat brain membranes

3H-dihydroergotamine, which is used clinically to treat orthostatic hypotension and migraine, binds saturably, reversibly and with high affinity (K D = 0.2 nM) to rat brain membranes. The binding is time, temperature and pH dependent and is highest in the hippocampus and the corpus striatum. Seroton...

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Veröffentlicht in:	Life sciences (1973) 1976-12, Vol.19 (12), p.1851-1864
Hauptverfasser:	Closse, Annemarie, Hauser, Daniel
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Binding, Competitive Brain - ultrastructure Cations, Divalent - pharmacology Dihydroergotamine - metabolism Ergot Alkaloids - metabolism Ergotamines Heart Hydrogen-Ion Concentration Kinetics Male Rats Serotonin - metabolism Stereoisomerism Structure-Activity Relationship Subcellular Fractions - metabolism
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Zusammenfassung:	3H-dihydroergotamine, which is used clinically to treat orthostatic hypotension and migraine, binds saturably, reversibly and with high affinity (K D = 0.2 nM) to rat brain membranes. The binding is time, temperature and pH dependent and is highest in the hippocampus and the corpus striatum. Serotonin was the only neurotransmitter tested capable of inhibiting 3H-DHE binding.
ISSN:	0024-3205 1879-0631
DOI:	10.1016/0024-3205(76)90117-X