k Opioids as potential treatments for stimulant dependence

Prisinzano, Thomas E.; Tidgewell, Kevin; Harding, Wayne W.

doi:10.1208/aapsj070361

Cited by 72 publications

(76 citation statements)

References 119 publications

(84 reference statements)

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“…Esta substância parece ser "alucinógeno por excelência" (Valdes, 1994), produzindo efeitos psicotrópicos apenas pela estimulação do receptor opióide kappa (González et al, 2006;Prisinzano, 2005;Babu et al, 2008), com afinidade muito pouco significativa pelos receptores opióides mu (Wang et al, 2004;Rothman et al, 2007) e kappa do tipo 2 (Ansonoff et al, 2006) e sem ação sobre receptores serotoninérgicos do tipo 2A (González et al, 2006;Prisinzano, 2005;Babu et al, 2008).…”

Section: Revisãounclassified

“…Classicamente a "hipótese dopaminérgica" tem sido usada para explicar adição e dependência de substâncias (Prisinzano et al, 2005). SA e outros agonist as kappa-opi ói des diminuem significativamente os níveis basais de dopamina, assim como impedem o aumento dos níveis dopaminérgicos (Prisinzano et al, 2005).…”

Section: Mecanismo De Ação Da Salvinorina a E Relação Com Potencial Dunclassified

“…SA e outros agonist as kappa-opi ói des diminuem significativamente os níveis basais de dopamina, assim como impedem o aumento dos níveis dopaminérgicos (Prisinzano et al, 2005). Pesquisa-se o uso de agonistas seletivos de KOP no tratamento da dependência por estimulantes (Prisinzano et al, 2005;Chefer et al, 2005). Parece também atuar como eficiente bloqueador do efeito de recompensa provocado por morfina (Narita et al, 2005), levando em conta que o KOP participa da expressão da síndrome de abstinência crônica induzida por aquele opióide (Lee et al, 2005).…”

Section: Mecanismo De Ação Da Salvinorina a E Relação Com Potencial Dunclassified

“…Pode-se prever crescimento rápido do uso abusivo de SDI e SA (Prisinzano, 2005). Apenas um levantamento epidemiológico define perfil de idade e gênero para o primeiro uso da SDI e o consumo no último mês, no norte da Itália (Tabela 1) (Pavarin, 2006).…”

Section: Figura 1 Estrutura De Dois Terpenóides De Mesmo Perfil Farmunclassified

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Salvia divinorum Epling & Játiva (Maria Pastora) e Salvinorina A: crescente uso recreacional e potencial de abuso

Schneider

Ardenghi

2010

Rev. bras. plantas med.

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RESUMO:A planta Salvia divinorum Epling & Játiva (SDI), da família Lamiaceae, tem sido usada por séculos pela cultura mazateca e vem ganhando popularidade como droga recreacional nos últimos anos. Seu princípio ativo -Salvinorina A (SA) -é agonista dos receptores opióides kappa, com potencial psicotrópico. A utilização da planta vem crescendo na Europa e na América do Norte, apesar de ainda não existirem provas concretas sobre abuso. A presente revisão da literatura contemporânea aborda as evidências sobre o potencial de abuso de SDI, bem como o crescente uso recreacional, ainda que seja alucinógeno permitido legalmente e de fácil compra em muitos países.

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Section: Revisãounclassified

Section: Mecanismo De Ação Da Salvinorina a E Relação Com Potencial Dunclassified

Section: Figura 1 Estrutura De Dois Terpenóides De Mesmo Perfil Farmunclassified

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Salvia divinorum Epling & Játiva (Maria Pastora) e Salvinorina A: crescente uso recreacional e potencial de abuso

Schneider

Ardenghi

2010

Rev. bras. plantas med.

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Multiple OPR genes influence personality traits in substance dependent and healthy subjects in two American populations

Luο

Zuo

Kranzler

et al. 2008

American J of Med Genetics Pt B

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Background Personality traits are among the most complex quantitative traits. Certain personality traits are associated with substance dependence (SD); genetic factors may influence both. Associations between opioid receptor (OPR) genes and SD have been reported. This study investigated the relationship between OPR genes and personality traits in a case-control sample. Methods We assessed dimensions of the five-factor model of personality in 556 subjects: 250 with SD [181 European-Americans (EAs) and 69 African-Americans (AAs)] and 306 healthy subjects (266 EAs and 40 AAs). We genotyped 20 OPRM1 markers, 8 OPRD1 markers, and 7 OPRK1 markers, and 38 unlinked ancestry-informative markers in these subjects. The relationships between OPR genes and personality traits were examined using MANCOVA, controlling for gene-gene interaction effects and potential confounders. Associations were decomposed by Roy-Bargmann Stepdown ANCOVA. Results Personality traits were associated as main or interaction effects with the haplotypes, diplotypes, alleles and genotypes at the three OPR genes (0.002

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Quantum Dot‐Based Screening System for Discovery of G Protein‐Coupled Receptor Agonists

et al. 2012

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Cellular imaging has emerged as an important tool to unravel biological complexity and to accelerate the drug-discovery process, including cell-based screening, target identification, and mechanism of action studies. Recently, semiconductor nanoparticles known as quantum dots (QDs) have attracted great interest in cellular imaging applications due to their unique photophysical properties such as size, tunable optical property, multiplexing capability, and photostability. Herein, we show that QDs can also be applied to assay development and eventually to high-throughput/content screening (HTS/HCS) for drug discovery. We have synthesized QDs modified with PEG and primary antibodies to be used as fluorescent probes for a cell-based HTS system. The G protein-coupled receptor (GPCR) family is known to be involved in most major diseases. We therefore constructed human osteosarcoma (U2OS) cells that specifically overexpress two types of differently tagged GPCRs: influenza hemagglutinin (HA) peptide-tagged κ-opioid receptors (κ-ORs) and GFP-tagged A3 adenosine receptors (A3AR). In this study, we have demonstrated that 1) anti-HA antibody-conjugated QDs could specifically label HA-tagged κ-ORs, 2) subsequent treatment of QD-tagged GPCR agonists allowed agonist-induced translocation to be monitored in real time, 3) excellent emission spectral properties of QD permitted the simultaneous detection of two GPCRs in one cell, and 4) the robust imaging capabilities of the QD-antibody conjugates could lead to reproducible quantitative data from high-content cellular images. These results suggest that the present QD-based GPCR inhibitor screening system can be a promising platform for further drug screening applications.

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k Opioids as potential treatments for stimulant dependence

Cited by 72 publications

References 119 publications

Salvia divinorum Epling & Játiva (Maria Pastora) e Salvinorina A: crescente uso recreacional e potencial de abuso

Salvia divinorum Epling & Játiva (Maria Pastora) e Salvinorina A: crescente uso recreacional e potencial de abuso

Multiple OPR genes influence personality traits in substance dependent and healthy subjects in two American populations

Quantum Dot‐Based Screening System for Discovery of G Protein‐Coupled Receptor Agonists

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