u-50488 has been researched along with morphine-6-glucuronide* in 2 studies
2 other study(ies) available for u-50488 and morphine-6-glucuronide
| Article | Year |
|---|---|
Lack of mu-opioid receptor-mediated G-protein activation in the spinal cord of mice lacking Exon 1 or Exons 2 and 3 of the MOR-1 gene.
The G-protein activation induced by mu-opioid receptor agonists was determined in spinal cord membranes from two types of mu-opioid receptor knockout mice: mice with a disruption of exon 1 (MOR (Exon 1)-KO) or exons 2 and 3 (MOR (Exons 2 and 3)-KO) of the mu-opioid receptor gene. The G-protein activation induced by the opioid agonists was measured by monitoring the increases of guanosine-5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTP gamma S) binding. The mu-opioid receptor agonists (D-Ala(2),N-MePhe (4),Gly-ol(5)]enkephalin, endomorphin-1, endomorphin-2, morphine, morphine-6 beta-glucuronide, and fentanyl produced concentration-dependent increases of [(35)S]GTP gamma S binding to spinal cord membranes in wild-type mice, but not in MOR (Exon 1)-KO mice or MOR (Exons 2 and 3)-KO mice. On the other hand, the delta-opioid receptor agonist [D-Pen (2,5)]enkephalin, the kappa-opioid receptor agonist (-)U50,488H, or the ORL1-receptor agonist nociception increased [(35)S]GTP gamma S binding in the spinal cord membranes from both MOR (Exon 1)-KO mice and MOR (Exons 2 and 3)-KO mice to the same extent as in the corresponding wild-type mice. The results provide further information about the important roles of the sequences encoded within exon 1 and exons 2 and 3 of mu-opioid receptor gene for the activation of G-proteins by mu-opioid receptor agonists in the mouse spinal cord. Topics: 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; Animals; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, D-Penicillamine (2,5)-; Exons; Fentanyl; GTP-Binding Proteins; Guanosine 5'-O-(3-Thiotriphosphate); In Vitro Techniques; Mice; Mice, Knockout; Morphine Derivatives; Nociceptin; Nociceptin Receptor; Oligopeptides; Opioid Peptides; Radioligand Assay; Receptors, Opioid; Receptors, Opioid, delta; Receptors, Opioid, kappa; Receptors, Opioid, mu; Spinal Cord | 2003 |
The antinociceptive and motivational effects of intranigral injection of opioid agonists.
The antinociceptive potency of morphine and the morphine metabolite morphine-6-glucuronide (M6G) was examined after injection into the substantia nigra and periaqueductal gray (PAG) of rats. Both drugs produced antinociception in both sites. The antinociceptive potency of M6G was significantly greater than morphine in the nigra. There was no difference in the antinociceptive potency of M6G in the nigra and PAG. M6G and other opioids were also examined for motivational effects after intranigral injection. A high dose of intranigral morphine (10.0 nmol) produced a conditioned place preference. No significant motivational effects were produced by 1.0 nmol of M6G, D-Ala2, N-Me-Phe4,Gly5-ol-enkephalin (DAGO), D-Pen2,D-Pen5-enkephalin (DPDPE), or U-50,488H. It is concluded that the substantia nigra plays an important role in opioid antinociception. The role of the nigra in opioid reward is questionable. Topics: 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; Analgesics; Analysis of Variance; Animals; Dose-Response Relationship, Drug; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, D-Penicillamine (2,5)-; Enkephalins; Male; Microinjections; Morphine; Morphine Derivatives; Motivation; Pain; Periaqueductal Gray; Pyrrolidines; Rats; Rats, Sprague-Dawley; Reward; Stereotaxic Techniques; Substantia Nigra; Time Factors | 1993 |