Abstract
mu opiate receptors recognize morphine with high affinity. A 2.1-kb rat brain cDNA whose predicted translation product displays 63% identity with recently described delta and kappa opiate receptor sequences was identified through polymerase chain reaction and cDNA homology approaches. This cDNA recognizes a 10.5-kb mRNA that is expressed in thalamic neurons. COS-cell expression confers naloxonazine-, Na(+)-, and GTP-sensitive binding of mu but not delta or kappa opioid ligands. Expressing cells bind morphine, [D-Ala2,N-methyl-Phe4,glyol5]enkephalin (DAMGO), and [D-Ala2,D-Leu5]enkephalin (DADLE) with nanomolar or subnanomolar affinities, defining a mu opiate receptor that avidly recognizes analgesic and euphoric opiate drugs and opioid peptides.
MeSH terms
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Amino Acid Sequence
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Animals
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Base Sequence
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Brain / metabolism*
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Cloning, Molecular
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DNA Primers
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DNA, Complementary / chemistry
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DNA, Complementary / metabolism*
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Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
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Enkephalin, Leucine-2-Alanine / metabolism
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Enkephalins / metabolism
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Escherichia coli
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Gene Expression
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Humans
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Kinetics
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Molecular Sequence Data
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Polymerase Chain Reaction
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Protein Biosynthesis
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RNA, Messenger / biosynthesis
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RNA, Messenger / isolation & purification
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Rats
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Receptors, Opioid, mu / biosynthesis*
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Receptors, Opioid, mu / isolation & purification
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Receptors, Opioid, mu / metabolism
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Recombinant Proteins / metabolism
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Sequence Homology, Amino Acid
Substances
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DNA Primers
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DNA, Complementary
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Enkephalins
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RNA, Messenger
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Receptors, Opioid, mu
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Recombinant Proteins
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Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
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Enkephalin, Leucine-2-Alanine