Blockade of neuronal m-channels as a therapeutic approach to the

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514256, 514315, 514430, 514449, A61K 3150, A61K 31505, A61K 31445, A61K 3138

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active

057505284

ABSTRACT:
Compounds which block neuronal M-channels are useful for treating conditions involving neurotransmitter deficiencies, traumatic brain injury, or the depressive phase of bipolar disorder. Compounds can be evaluated for utility in treating these conditions by determining whether they are capable of blocking neuronal M-channels.

REFERENCES:
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Frey et al., DuP996, a Novel Neurotransmitter Releaser, Blocks Voltage-Activated Potassium Currents in Cultured Neocortical Neurons, Soc. Neuroscience Abstr., 17 1588, Abstract #632.20 (1991).
Aiken and Brown, Linopirdine (DuP 996), A Neurotransmitter Release Enhancer, Blocks M-Current in Rat CA1 Hippocampal Neurons, Biophy.J. 66:A210 (1994) Tu-Pos 410 and Brain Research Assoc. Abstracts 11:67, Abstract #17.200 (1994).
Maciag, et al., Studies on the Role of K+, Cl-, and Na+ Ion Permeabilities in the Acetylcholine Release Enhancing Effects of Linopirdine (DuP 996) in Rat Cerebral Cortical Slices, J. Pharmacol. Exper. Therapy, 271, 891-897 (1994).
Aiken, et al., Reduction of Spike Fequency Adaptation and Blockade of M-Current in Rat CA1 Pyramidal Neurones by Linopirdine (DuP 996), a Neurotransmitter Release Enhancer, Br.J.Pharmacol.115, 1163-1168 (1995).

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