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• W2417863669 abstract "Physiological studies suggest that the formamidine pesticides, chlordimeform (CDM) and N-demethylchlordimeform (DCDM), may affect octopaminergic neurotransmission. To elucidate the possible mechanism of this interaction, the present study examined in detail the biochemical effects of these compounds on a very active octopamine-sensitive adenylate cyclase present in washed particulate preparations of the firefly light organ. DCDM was a partial agonist (70% of octopamine Vmax) and was 6-fold more potent (Ka = 2.2 x 10-6 M) than octopamine (Ka = 1.4 x 10-5 M) in activating enzyme activity. At high concentrations (IC50 = 3 x 10-4 M), DCDM caused a 30% inhibition of octopamine stimulation. Activation by DCDM was reversible, nonadditive to that caused by octopamine, and could be competitively inhibited by several receptor antagonists, including cyproheptadine (Ki = 2 x 10-6 M), clozapine (Ki = 4 x 10-6 M), fluphenazine (Ki = 6 x 10-6 M), phentolamine (Ki = 1.8 x 10-5 M), and propranolol (Ki = 4.7 x 10-5 M). These inhibitory constants correlated well with those for inhibiting octopamine stimulation. The agonist activity of DCDM was specific for tissue containing an octopamine-activated adenylate cyclase; enzyme activity in the rat caudate nucleus (activated by dopamine) and in the heart and liver (activated by isoproterenol) was little affected by DCDM. In contrast to DCDM, CDM was a weak octopamine agonist (Ka = 3 x 10-5 M; 9% of octopamine Vmax) in the light organ. At higher concentrations (IC50 = 3 to 10 x 10-4 M), CDM was an octopamine antagonist, causing nearly complete inhibition of octopamine stimulation at 1 to 3 x 10-3 M. This inhibitory effect of CDM was reversible, pH-dependent, and noncompetitive with octopamine. It was also nonselective, since CDM inhibited dopamine-sensitive, beta-adrenergic-sensitive, and non-hormone-dependent adenylate cyclases in mammalian brain and liver. The above results indicate that, at low concentrations, DCDM can bind specifically and reversibly to octopamine receptors with a resultant activation of adenylate cyclase. CDM, on the other hand, has little direct effect on the octopamine receptor; its octopamimetic actions in vivo are a probable result of its conversion to DCDM. At high, nonpharmacological doses, CDM exerts noncompetitive and non-receptor-specific inhibitory effects on adenylate cyclase. These data have relevance to understanding the structural requirements necessary for interaction with octopamine-sensitive adenylate cyclase." @default.
• W2417863669 created "2016-06-24" @default.
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• W2417863669 date "1981-07-01" @default.
• W2417863669 modified "2023-09-25" @default.
• W2417863669 title "N-demethylchlordimeform: a potent partial agonist of octopamine-sensitive adenylate cyclase." @default.
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