ISSN:
0739-4462
Schlagwort(e):
[N-methyl-3H]mianserin
;
cockroach nerve cord
;
octopamine receptor
;
cyclic AMP
;
Chemistry
;
Food Science, Agricultural, Medicinal and Pharmaceutical Chemistry
Quelle:
Wiley InterScience Backfile Collection 1832-2000
Thema:
Biologie
Notizen:
The binding of [3H]mianserin to homogenates of cockroach nerve cord was investigated, using a centrifugal binding assay. Nonspecific binding was defined as binding in the presence of 0.1 μM phentolamine. Specific binding was saturable and indicated a high affinity site (KD = 39.6 nM and Bmax = 0.8 fmol μGg-1) and a low affinity site (KD = 648.9 nM and Bmax = 5.9 fmol μg-1). The binding was reduced or abolished by heat, detergents, trypsin and HgCl2. Incorporation of CaCl2 or NaCl into the medium reduced binding in a dose-dependent fashion, whereas MgCl2 and NaF inhibited binding in a biphasic manner. The stable GTP analog, 5′-guanylylimidodiphosphate, reduced the high affinity binding at 10 μM. Phentolamine, D,L-octopamine, demethylchlordimeform (DCDM), clonidine, and D,L-synephrine are effective displacers of [3H]mianserin-binding, whereas dopamine, acetylcholine, serotonin (5-HT), and histamine show poor or no displacement. The pharmacological properties of octopamine-sensitive adenylate cyclase stimulation in cockroach nerve cord are similar to those of [3H]mianserin-binding.
Zusätzliches Material:
4 Ill.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1002/arch.940060307
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