摘要:
The present disclosure provides organophosphorous (OP) compounds of Formula (I), Formula (II) and Formula (III): OP-Peptide-Linker-CP (I), OP-Peptide-Linker (II); and wherein OP is including that structure corresponding to a reactive organophosphorous reagent, nerve agent or pesticide, or a pesticide P═S to P═O metabolite; P is the Sp or Rp stereoisomer; X is oxygen, sulfur, selenium or imino; R and R′ are as described; Peptide is a sequence of amino acids containing a serine, threonine or tyrosine to which the OP is attached, wherein the total number of amino acids is between 7 and 41; Linker is an amino acid or is derived from another bifunctional reagent capable of covalently attaching an OP-peptide to a CP; and CP is a carrier protein used to display haptens for antibody generation. The disclosure also provides methods for generating monoclonal or polyclonal antibodies specific for an OP-Peptide of a compound of Formula (I) or Formula (II) that can be used to diagnose the presence, identity, and quantity of OP adducts.
摘要:
The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.
摘要:
Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.
摘要:
The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.
摘要:
Disclosed herein are compounds of formula (I); as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using these compounds for the treatment of substance addiction.
摘要:
Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.
摘要:
Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.
摘要:
Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, ALS, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for evaluation in animal models of neurodegenerative diseases.
摘要:
Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for use in animal models of neurodegenerative diseases.