Title : The dual modulation of GIRK1/GIRK2 channels by opioid receptor ligands.

Pub. Date : 1999 Dec 3

PMID : 10607882






7 Functional Relationships(s)
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1 It is well known that activation of the cloned kappa-opioid receptor by nanomolar concentrations of U50488H (trans-(+/-)-3, 4-dichloro-N-methyl-N-(2-[1-pyrrolidinyl]cyclohexyl-benzeneacetamide) , a selective kappa-opioid receptor agonist, leads to the opening of GIRK1 channels. 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer potassium inwardly rectifying channel subfamily J member 3 Homo sapiens
2 It is well known that activation of the cloned kappa-opioid receptor by nanomolar concentrations of U50488H (trans-(+/-)-3, 4-dichloro-N-methyl-N-(2-[1-pyrrolidinyl]cyclohexyl-benzeneacetamide) , a selective kappa-opioid receptor agonist, leads to the opening of GIRK1 channels. 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer potassium inwardly rectifying channel subfamily J member 3 Homo sapiens
3 We also show that micromolar concentrations of U50488H reduce GIRK1/GIRK2 current through direct GIRK1/GIRK2 channel block in a voltage-independent manner (IC(50)=70.28+/-3.68 microM). 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer potassium inwardly rectifying channel subfamily J member 3 Homo sapiens
4 We also show that micromolar concentrations of U50488H reduce GIRK1/GIRK2 current through direct GIRK1/GIRK2 channel block in a voltage-independent manner (IC(50)=70.28+/-3.68 microM). 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer potassium inwardly rectifying channel subfamily J member 3 Homo sapiens
5 Similarly, it was found that propoxyphene, methadone, and naloxone also can block GIRK1/GIRK2 current. Dextropropoxyphene potassium inwardly rectifying channel subfamily J member 3 Homo sapiens
6 Similarly, it was found that propoxyphene, methadone, and naloxone also can block GIRK1/GIRK2 current. Methadone potassium inwardly rectifying channel subfamily J member 3 Homo sapiens
7 Similarly, it was found that propoxyphene, methadone, and naloxone also can block GIRK1/GIRK2 current. Naloxone potassium inwardly rectifying channel subfamily J member 3 Homo sapiens