ABSTRACT
A rat brain cDNA library was screened with probes constructed from portions of the cDNA (OBCAM) encoding the opioid-binding cell adhesion molecule (OBCAM). Three clones of interest were isolated and sequenced. The largest clone, DUZ1, had a putative open reading frame (ORF) essentially identical to OBCAM in its C-terminal 318 amino acids (aa), but differing in its N-terminal aa (20 vs. 27 in OBCAM), and in all of its 5'-noncoding regions. The other clones, SG8 and SG13, had a putative ORF essentially identical to that of OBCAM, but differed from each other in a portion of their 5'-noncoding region. This study suggests that there is a family of OBCAM-like genes.
Subject(s)
Multigene Family/genetics , Receptors, Opioid/genetics , Amino Acid Sequence , Animals , Base Sequence , Cloning, Molecular , DNA/genetics , Gene Library , Molecular Sequence Data , Rats , Receptors, Opioid/chemistry , Receptors, Opioid, deltaABSTRACT
The opioid agonist and antagonist effects of two configurational aminotetralin stereoisomers, namely, the cis-(MRSAL) and trans-(RMG) diastereo isomers of 3-(dimethylamino)-2,2-dimethyl-7-hydroxy-1-tetralol were studied using the guinea pig ileum longitudinal muscle preparation. MRSAL demonstrated opioid antagonist activity but failed to show agonist effects. In contrast, RMG showed agonist activity which was partially reversed by NX and MRSAL. RMG also exhibited weak antagonist activity towards DHM, NM and DADLE. These results showed that MRSAL was an opioid antagonist while RMG possessed weak mixed opioid agonist-antagonist activities.
Subject(s)
Muscle Contraction/drug effects , Naphthalenes/pharmacology , Narcotic Antagonists/pharmacology , Narcotics/pharmacology , Tetrahydronaphthalenes/pharmacology , Tetralones , Animals , Electric Stimulation , Guinea Pigs , Ileum/drug effects , Ileum/physiology , In Vitro Techniques , Male , StereoisomerismABSTRACT
Two substituted analogs of 3-amino-2,2-dimethyltetralin, namely 3-dimethylamino-2,2-dimethyl-7-hydroxy-1-tetralone HBr (J) and 3-dimethylamino-2,2-dimethyl-7-hydroxy-1-tetralol (MRSAL), were evaluated for opioid agonist and antagonist activity using the electrically driven guinea pig ileum longitudinal muscle preparation (GPI). Compound J appeared to be an opioid agonist with a preference for mu receptors while MRSAL was an opioid antagonist with little selectivity for mu or kappa receptors.
