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Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands. 2002

Wen-Lian Wu, and Mary Ann Caplen, and Martin S Domalski, and Hongtao Zhang, and Ahmad Fawzi, and Duane A Burnett
Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA.

A series of aminoalkylazetidines has been discovered as novel ORL1 receptor ligands. Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified.

UI MeSH Term Description Entries
D007202 Indicators and Reagents Substances used for the detection, identification, analysis, etc. of chemical, biological, or pathologic processes or conditions. Indicators are substances that change in physical appearance, e.g., color, at or approaching the endpoint of a chemical titration, e.g., on the passage between acidity and alkalinity. Reagents are substances used for the detection or determination of another substance by chemical or microscopical means, especially analysis. Types of reagents are precipitants, solvents, oxidizers, reducers, fluxes, and colorimetric reagents. (From Grant & Hackh's Chemical Dictionary, 5th ed, p301, p499) Indicator,Reagent,Reagents,Indicators,Reagents and Indicators
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D009292 Narcotic Antagonists Agents inhibiting the effect of narcotics on the central nervous system. Competitive Opioid Antagonist,Narcotic Antagonist,Opioid Antagonist,Opioid Antagonists,Opioid Receptor Antagonist,Opioid Reversal Agent,Competitive Opioid Antagonists,Opioid Receptor Antagonists,Opioid Reversal Agents,Agent, Opioid Reversal,Agents, Opioid Reversal,Antagonist, Competitive Opioid,Antagonist, Narcotic,Antagonist, Opioid,Antagonist, Opioid Receptor,Antagonists, Competitive Opioid,Antagonists, Narcotic,Antagonists, Opioid,Antagonists, Opioid Receptor,Opioid Antagonist, Competitive,Opioid Antagonists, Competitive,Receptor Antagonist, Opioid,Receptor Antagonists, Opioid,Reversal Agent, Opioid,Reversal Agents, Opioid
D011957 Receptors, Opioid Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known. Endorphin Receptors,Enkephalin Receptors,Narcotic Receptors,Opioid Receptors,Receptors, Endorphin,Receptors, Enkephalin,Receptors, Narcotic,Receptors, Opiate,Endorphin Receptor,Enkephalin Receptor,Normorphine Receptors,Opiate Receptor,Opiate Receptors,Opioid Receptor,Receptors, Normorphine,Receptors, beta-Endorphin,beta-Endorphin Receptor,Receptor, Endorphin,Receptor, Enkephalin,Receptor, Opiate,Receptor, Opioid,Receptor, beta-Endorphin,Receptors, beta Endorphin,beta Endorphin Receptor,beta-Endorphin Receptors
D004174 Diprenorphine A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine. Diprenorphine Hydrochloride,Revivon,Hydrochloride, Diprenorphine
D006224 Cricetinae A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS. Cricetus,Hamsters,Hamster
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000094942 Nociceptin Receptor A member of the opioid subfamily of the G PROTEIN-COUPLED RECEPTORS. It is the receptor for the endogenous neuropeptide nociceptin. It functions in modulating NOCICEPTION and the perception of pain. KOR-3 Protein,Kappa3-Related Opioid Receptor,MOR-C Protein,Nociceptin Receptors,OFQ Receptor,OFQ Receptors,ORL1 Receptor,ORL1 Receptors,Opiate Receptor-Like 1,Opioid Receptor-Like Protein,Opioid-Receptor-Like 1 Protein,Orphanin FQ Receptor,Orphanin FQ Receptors,Receptor, Nociceptin,Receptor, OFQ,Receptor, Orphanin FQ,Receptors, ORL1,Noci-R,1 Protein, Opioid-Receptor-Like,1, Opiate Receptor-Like,FQ Receptor, Orphanin,FQ Receptors, Orphanin,MOR C Protein,Noci R,Opioid Receptor Like 1 Protein,Protein, KOR-3,Protein, MOR-C,Protein, Opioid Receptor-Like,Protein, Opioid-Receptor-Like 1,Receptor, Kappa3-Related Opioid,Receptor-Like 1, Opiate,Receptor-Like Protein, Opioid,Receptors, Nociceptin,Receptors, Orphanin FQ
D000097629 Nociceptin A pronociceptive peptide that acts as a specific endogenous agonist to the NOCICEPTIN RECEPTOR. N-OFQ Peptide,Nociceptin-Orphanin FQ,Orphanin FQ
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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