摘要:
Tropane derivatives having a high binding affinity and selectivity for dopamine transporters bear, on the tropane backbone either a carboxylic ester or isoxazole moiety, as well as a substituted phenyl moiety. The compounds have utility both as pharmaceutical and as imaging agents, when one or more atoms are radioactive.
摘要:
Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CONRR.sub.2, R.sub.1 =hydrogen, C.sub.1-5 alkyl,X=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido,R and R.sup.2 may be saturated or unsaturated substituents of 1-6 carbon atoms, aromatic, or combine to form pyrrolidinyl, morpholinyl or piperidinyl moieties, andZ=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl, NR.sub.4 R.sub.5, NHCOF.sub.5, NHCO.sub.2 R.sub.6,wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.
摘要翻译:新型化合物对脑中特定的可卡因受体,特别是多巴胺转运蛋白位点表现出高亲和力,并且具有下式:其中Y = CONRR2,R1 =氢,C1-5烷基,X = H,C1-6烷基,C3- 8环烷基,C 1-4烷氧基,C 1-6炔基,卤素,氨基,酰基酰氨基,R和R 2可以是1-6个碳原子的饱和或不饱和取代基,芳族或结合形成吡咯烷基,吗啉基或哌啶基部分,Z = H,I,Br,Cl,F,CN,CF 3 NO 2,N 3,OR 1,CO 2 NH 2,CO 2 R 1,C 1-6烷基,NR 4 R 5,NHCOF 5,NHCO 2 R 6,其中R 4 -R 6各自为C 1-6烷基。
摘要:
This invention relates to novel compositions, their preparation and the use thereof as anticholinergic agents in the treatment or prophylaxis of organophosphate or nerve gas poisoning in animals. These compositions and pharmaceutical preparations containing them in their free base form and acid addition salts thereof are represented by the formula ##STR1## wherein R represents lower alkyl groups containing 1 to 7 carbon atoms; R.sup.1 represents hydrogen, phenyl, cyclohexyl, and cyclopentyl; and R.sup.2 represents lower alkyl groups containing 1 to 7 carbon atoms, hydroxymethyl, and hydroxyl.
摘要:
Methods and apparatus to improve throughput and efficiency in memory devices are described. In one embodiment, a memory controller may include scheduler logic to issue read or write requests to a memory device in an optimal fashion, e.g., to maximize bandwidth and/or reduce latency. Other embodiments are also disclosed and claimed.
摘要:
The invention generally relates to hapten compounds comprising either (+) methamphetamine or (+) amphetamine conjugated to a linker. Generally speaking, hapten compounds of the invention may be used to elicit an immune response to one or more of (+) methamphetamine, (+) amphetamine, or (+) MDMA.
摘要:
The present invention is related to antibodies directed to various drugs of abuse and uses of such antibodies. In preferred embodiments, the drugs of abuse are amphetamine, methamphetamine, or phencyclidine (PCP). In particular, in accordance with the present invention, there are provided fully man monoclonal antibodies directed to drugs of abuse. Nucelotide sequences encoding, and amino acid sequences comprising, heavy and light chain immunoglobulin molecules, particularly sequences corresponding to contiguous heavy and light chain sequences spanning the framework regions and/or complementarity determining regions (CDR's), specifically from FR1 through FR3 or CDR1 through CDR3, are provided. Hybridomas or other cell lines expressing such immunoglobulin molecules and monoclonal antibodies are also provided.
摘要:
The invention includes synthetic immunochemical haptens for the generation of antibodies, the antibodies, and the medical treatment applications for using the antibodies. The antibodies are designed to recognize the common molecular features of d-methamphetamine-like abused stimulants, and will have insignificant cross-reactivity with endogenous substrates (e.g. dopamine) or over-the-counter medications (e.g. 1-methamphetamine, pseudoephedrine, phenylpropanolamine and ephedrine). These monoclonal antibodies and their antigen binding fragments are useful in treatment plans for recovering addicts, in emergency room settings for rapidly reversing a drug overdose, in protection of fetuses or fetus from drug-abusing pregnant mothers or in a psychiatric setting to reduce the exacerbation of psychotic disorders caused by stimulant drugs.
摘要:
Systems, methods, and apparatuses relating to circuitry to implement lockstep of processor cores are described. In one embodiment, a hardware processor comprises a first processor core comprising a first control flow signature register and a first execution circuit, a second processor core comprising a second control flow signature register and a second execution circuit, and at least one signature circuit to perform a first state history compression operation on a first instruction that executes on the first execution circuit of the first processor core to produce a first result, store the first result in the first control flow signature register, perform a second state history compression operation on a second instruction that executes on the second execution circuit of the second processor core to produce a second result, and store the second result in the second control flow signature register.
摘要:
The invention provides bupropion analog compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.