Abstract: The present invention relates to a novel mammalian met one-specific opioid receptor protein and genes that encode a such protein. The invention is directed toward the isolation, characterization and pharmacological use of mammalian methadone-specific opioid receptor proteins. The invention specifically provides isolated complementary DNA copies of mRNA corresponding to the rat homologue or the mammalian methadone-specific opioid receptor gene. Also provided are recombinant expression constructs capable of expressing the mammalian methadone-specific opioid receptor genes of the invention in cultures of transformed prokaryotic and eukaryotic cells, as well as such cultures of transformed cells that synthesize the mammalian methadone-specific opioid receptor proteins encoded therein.

Abstract: The present invention relates to a novel mammalian anti-opioid receptor protein (OFQR), peptide ligands (such as OFQ) that bind to OFQR, and methods of using the OFQ peptide and analogues to reverse the physiologic effects of opiates such as morphine. The isolation, characterization and pharmacological use of the endogenous peptide ligand is described. A particular embodiment of the OFQ peptide is a heptadecapeptide having an FGGF aminoterminal motif. The peptide specifically binds to an OFQ receptor protein heterologously expressed in mammalian cells. The peptide does not bind with high affinity to .mu., .delta. or .kappa. receptors, but it antagonizes opioid mediated effects (such as analgesia and hypothermia) without increasing nociceptive sensitivity. Tyrosine substitution variants of the peptide ligand specifically bind to the opioid receptor and can be radioiodinated.

Abstract: The present invention relates to the isolation, characterization and pharmacological uses for the human D5 dopamine receptor, the gene corresponding to this receptor, pseudogenes of this receptor gene, a recombinant eukaryotic expression vector capable of expressing the human D5 dopamine receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that synthesize the human D5 dopamine receptor. The invention relates to the biochemical and physiological characterization of the human D5 dopamine receptor and the development and testing of drugs useful for treating or preventing human disease.

Abstract: The present invention relates to a novel mammalian methadone-specific opioid receptor protein and genes that encode a such protein. The invention is directed toward the isolation, characterization and pharmacological use of mammalian methadone-specific opioid receptor proteins. The invention specifically provides isolated complementary DNA copies of mRNA corresponding to the rat homologue or the mammalian methadone-specific opioid receptor gene. Also provided are recombinant expression constructs capable of expressing the mammalian methadone-specific opioid receptor genes of the invention in cultures of transformed prokaryotic and eukaryotic cells, as well as such cultures of transformed cells that synthesize the mammalian methadone-specific opioid receptor proteins encoded therein.

Abstract: Cloned genes which code for the D.sub.1 dopamine receptor are disclosed. The receptors coded for by these clones bind dopamine ligands with the proper pharmacological profile and, when expressed in the cell membrane of a suitable host and so bound, stimulate adenylyl cyclase. Also disclosed are vectors comprising a cloned gene encoding a D.sub.1 -dopamine receptor, cells transformed with such vectors, and oligonucleotide probes capable of selectively hybridizing to DNA comprising a portion of a gene coding for a D.sub.1 -dopamine receptor. The cloned genes are useful for making proteins and cell membrane preparations which can be used to screen compounds for D.sub.1 -dopamine receptor binding activity, are useful in molecular biology, and are useful as diagnostic probes.

Abstract: The present invention is directed toward the isolation, characterization and pharmacological use of the human D4 dopamine receptor. The nucleotide sequence of the gene corresponding to this receptor and alleleic variants thereof are provided by the invention. The invention particularly provides recombinant eukaryotic expression constructs capable of expressing the human D4 dopamine receptor at useful levels in cultures of transformed eukaryotic cells. The invention provides cultures of transformed eukaryotic cells which synthesize such useful amounts of human D4 dopamine receptor protein, and methods for characterizing novel psychotropic compounds using such cultures.

Abstract: The present invention relates to the isolation, characterization and pharmacological uses for the human D5 dopamine receptor, the gene corresponding to this receptor, pseudogenes of this receptor gene, a recombinant eukaryotic expression vector capable of expressing the human D5 dopamine receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that synthesize the human D5 dopamine receptor. The invention relates to the biochemical and physiological characterization of the human D5 dopamine receptor and the development and testing of drugs useful for treating or preventing human disease.

Abstract: Cloned genes which code for the D.sub.1 dopamine receptor are disclosed. The receptors coded for by these clones bind dopamine ligands with the proper pharmacological profile and, when expressed in the cell membrane of a suitable host and so bound, stimulate adenylyl cyclase. Also disclosed are vectors comprising a cloned gene encoding a D.sub.1 -dopamine receptor, cells transformed with such vectors, and oligonucleotide probes capable of selectively hybridizing to DNA comprising a portion of a gene coding for a D.sub.1 -dopamine receptor. The cloned genes are useful for making proteins and cell membrane preparations which can be used to screen compounds for D.sub.1 -dopamine receptor binding activity, are useful in molecular biology, and are useful as diagnostic probes.