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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Scheer H W, Lavoie P A

Department of Pharmacology, University of Montreal, Canada.

Gen Pharmacol. 1991;22(1):169-72. doi: 10.1016/0306-3623(91)90329-5.

Aminopyridines (APs) induced the release of [3H]dopamine (3H-DA) from rat synaptosomal preparations. 2. 4-AP and 3,4-DAP were of equal efficacy in inducing release of 3H-DA; 3-AP, 2-AP and 2,6-AP were less active; pyridine and pyridine-4-carboxylamide were inactive. 3. Cd2+ was more effective in inhibiting 4-AP-induced release of 3H-DA (IC50 approximately 4 microM) than Co2+ and Ni2+ (IC50s approximately 500 microM). 4. While 4-AP increased the 45Ca2+ content of whole synaptosomal preparations, no effect of 4-AP on 45Ca2+ content was observed in lysed synaptosomal preparations. 5. 4-AP-induced 45Ca2+ uptake was inhibited by Cd2+, Ni2+ and Co2+ in concentration ranges similar to those inhibiting 3H-DA release.

氨基吡啶（APs）可诱导大鼠突触体制剂释放[3H]多巴胺（3H-DA）。2. 4-AP和3,4-DAP在诱导3H-DA释放方面具有同等效力；3-AP、2-AP和2,6-AP的活性较低；吡啶和吡啶-4-甲酰胺无活性。3. Cd2+在抑制4-AP诱导的3H-DA释放方面（IC50约为4 microM）比Co2+和Ni2+（IC50约为500 microM）更有效。4. 虽然4-AP增加了整个突触体制剂的45Ca2+含量，但在裂解的突触体制剂中未观察到4-AP对45Ca2+含量的影响。5. 4-AP诱导的45Ca2+摄取在与抑制3H-DA释放相似的浓度范围内受到Cd2+、Ni2+和Co2+的抑制。

Scheer H W, Lavoie P A

Department of Pharmacology, University of Montreal, Canada.

Gen Pharmacol. 1991;22(1):169-72. doi: 10.1016/0306-3623(91)90329-5.

Aminopyridines (APs) induced the release of [3H]dopamine (3H-DA) from rat synaptosomal preparations. 2. 4-AP and 3,4-DAP were of equal efficacy in inducing release of 3H-DA; 3-AP, 2-AP and 2,6-AP were less active; pyridine and pyridine-4-carboxylamide were inactive. 3. Cd2+ was more effective in inhibiting 4-AP-induced release of 3H-DA (IC50 approximately 4 microM) than Co2+ and Ni2+ (IC50s approximately 500 microM). 4. While 4-AP increased the 45Ca2+ content of whole synaptosomal preparations, no effect of 4-AP on 45Ca2+ content was observed in lysed synaptosomal preparations. 5. 4-AP-induced 45Ca2+ uptake was inhibited by Cd2+, Ni2+ and Co2+ in concentration ranges similar to those inhibiting 3H-DA release.

氨基吡啶（APs）可诱导大鼠突触体制剂释放[3H]多巴胺（3H-DA）。2. 4-AP和3,4-DAP在诱导3H-DA释放方面具有同等效力；3-AP、2-AP和2,6-AP的活性较低；吡啶和吡啶-4-甲酰胺无活性。3. Cd2+在抑制4-AP诱导的3H-DA释放方面（IC50约为4 microM）比Co2+和Ni2+（IC50约为500 microM）更有效。4. 虽然4-AP增加了整个突触体制剂的45Ca2+含量，但在裂解的突触体制剂中未观察到4-AP对45Ca2+含量的影响。5. 4-AP诱导的45Ca2+摄取在与抑制3H-DA释放相似的浓度范围内受到Cd2+、Ni2+和Co2+的抑制。