Ligands of the Mu, Kappa, and Delta Opioid Receptors
AssigneesThe Board of Trustees of the Leland Stanford Junior University, Memorial Sloan Kettering Cancer Center
InventorsEvan N. Feinberg, Vijay S. Pande, Susruta Majumdar, Gavril Pasternak
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Abstract
Ligands of the mu, kappa, and delta opioid receptors and methods of using them are disclosed. In particular, the invention relates to the discovery of new opioid receptor ligands based on molecular dynamics simulations of conformational states of the μ opioid receptor and the use of the identified opioid receptor ligands as analgesics, anti-diarrheal agents, and overdose reversal agents.
Claims28
A method of activating an opioid receptor, the method comprising contacting the opioid receptor with an effective amount of a composition comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), or 3,5-dimethyl-4-[6-(p-tolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
A method of treating pain in a subject, the method comprising administering a therapeutically effective amount of a composition comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), 3,5-dimethyl-4-[6-(p-tolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
A method of treating diarrhea in a subject, the method comprising administering a therapeutically effective amount of a composition comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), 3,5-dimethyl-4[6-(mtolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
A method of treating a drug overdose in a subject, the method comprising administering a therapeutically effective amount of a composition comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), 3,5-dimethyl-4-[6-(p-tolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
A composition for use in the treatment of pain comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), 3,5-dimethyl-4-[6-(p-tolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
A composition for use in the treatment of diarrhea comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), 3,5-dimethyl-4-[6-(p-tolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
A composition for use in the treatment of a drug overdose comprising 3,5-dimethyl-4-[6-(o-tolyloxy)hexyl]-1H-pyrazole (FMP4), 1-piperidino-5-(o-tolyloxy)pentane (FMP1), 3,5-dimethyl-4-[6-(p-tolyloxy)hexyl]-1H-pyrazole (FMP16), or a pharmaceutically acceptable salt thereof, or a combination thereof.
Dependencies are inferred from the claim text.