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Modulation of Ca 2+ Channels by Heterologously Expressed Wild-Type and Mutant Human μ-Opioid Receptors (hMORs) Containing the A118G Single-Nucleotide Polymorphism by Margas, Wojciech; Zubkoff, Ira; Schuler, H. Gregg; Janicki, Piotr K.; Ruiz-Velasco, Victor is a Neuroscience article available to read on EtoBox.
What is Modulation of Ca 2+ Channels by Heterologously Expressed Wild-Type and Mutant Human μ-Opioid Receptors (hMORs) Containing the A118G Single-Nucleotide Polymorphism about?
The most common single-nucleotide polymorphism (SNP) of the human μ-opioid receptor (hMOR) gene occurs at position 118 (A118G) and results in substitution of asparagine to aspartate at the N-terminus. The purpose of the present study was to compare the pharmacological profile of several opioid agonists to heterologously expressed hMOR and N-type Ca^2+^ channels in sympathetic neurons. cDNA constructs coding for wild-type and mutant hMOR were microinjected in rat superior cervical ganglion neurons and N-type Ca^2+^ channel modulation was investigated using the whole cell variant of the patch-clamp technique. Concentration–response relationships were generated with the following selective MOR agonists: DAMGO, morphine, morphine-6-glucuronide (M-6-G), and endomorphin I. The estimated maximal inhibition for the agonists ranged from 52 to 64% for neurons expressing either hMOR subtype. The rank order of potencies for estimated EC~50~ values (nM) in cells expressing wild-type hMOR was: DAMGO (31) ≫ morphine (76) ≅ M-6-G (77) ≅ endomorphin I (86). On the other hand, the rank order in mutant-expressing neurons was: DAMGO (14) ≫ morphine (39) ≫ endomorphin I (74) ≅ M-6-G (82), with a twofol
Who reads Modulation of Ca 2+ Channels by Heterologously Expressed Wild-Type and Mutant Human μ-Opioid Receptors (hMORs) Containing the A118G Single-Nucleotide Polymorphism?
It is typically read by researchers, students, and practitioners in Neuroscience.
- Author
- Margas, Wojciech; Zubkoff, Ira; Schuler, H. Gregg; Janicki, Piotr K.; Ruiz-Velasco, Victor
- Publisher
- The American Physiological Society; American Physiological Society (ISSN 0022-3077)
- Published
- 2007
- Language
- EN
- Field
- Neuroscience (Life Sciences)