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1.
Artigo | WPRIM (Pacífico Ocidental) | ID: wpr-835440

RESUMO

Purpose@#This study was performed to assess the accuracy of preoperative cone-beam computed tomography (CBCT), when justified for other reasons, in locating the apical foramen and establishing the working length. @*Materials and Methods@#Six electronic databases were searched for studies on this subject. All studies, of any type, were included if they compared measurements of working length with preoperative CBCT to measurements using an electronic apex locator (EAL) or histological reference standard. Due to the high levels of heterogeneity, an inverse-variance random-effects model was chosen, and weighted mean differences were obtained with 95% confidence intervals and P values. @*Results@#Nine studies were included. Compared to a histological reference standard, CBCT indicated that the apical foramen was on average 0.40 mm coronal of its histological position, with a mean absolute difference of 0.48 mm.Comparisons were also performed to an EAL reference standard, but the conclusions could not be considered robust due to high levels of heterogeneity in the results. @*Conclusion@#A low level of evidence is produced suggesting that preoperative CBCT shows the apical foramen to be on average 0.40 mm coronal to its histological position, with a mean absolute difference of 0.48 mm.

2.
Life Sci ; 82(11-12): 549-53, 2008 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-18261749

RESUMO

The compound (1R,2S/1S,2R)-2-[4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl) cyclopropanecarboxylate [(+/-)-PPCC] is a ligand with high affinity for sigma (sigma) sites of which the selectivity towards several other receptor systems has been demonstrated. Given the existence of a relationship between the sigma system and the kappa opioid (KOP)-mediated analgesia, to characterize the pharmacological properties of (+/-)-PPCC we analyzed its influence on the analgesic effect of the systemic injected kappa agonist (-)-U-50,488H comparing the effects with those shown by (+)-pentazocine and BD1047. The results demonstrate that the systemic administration of (+/-)-PPCC (1 mg/kg s.c.) does not modify basal tail-flick latency. Pre-treatment with (+/-)-PPCC, at the same dose, significantly decreased the antinociceptive effect of (-)-U-50,488H, analogously to the sigma compounds used. This study confirms that (+/-)-PPCC plays the role of sigma agonist in this model and strengthens the hypothesis of the sigma receptor modulatory role on KOP-mediated analgesia.


Assuntos
Analgésicos/metabolismo , Ciclopropanos/química , Ciclopropanos/metabolismo , Piperidinas/química , Piperidinas/metabolismo , Receptores Opioides kappa/metabolismo , Receptores sigma/metabolismo , (trans)-Isômero de 3,4-dicloro-N-metil-N-(2-(1-pirrolidinil)-ciclo-hexil)-benzenoacetamida/metabolismo , Animais , Ciclopropanos/farmacologia , Relação Dose-Resposta a Droga , Etilenodiaminas/metabolismo , Ligantes , Masculino , Estrutura Molecular , Medição da Dor , Pentazocina/metabolismo , Ratos , Ratos Sprague-Dawley , Receptores Opioides kappa/antagonistas & inibidores , Receptores sigma/antagonistas & inibidores
3.
J Med Chem ; 48(1): 266-73, 2005 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-15634021

RESUMO

In the attempt to define more accurately structure-affinity relationships for sigma(1) and sigma(2) ligands, we synthesized and tested on sigma subtype receptors a series of aralkyl derivatives of 4-benzylpiperidine, in which the effect of modifications on the aralkyl moiety was studied in a systematic way. The affinity of the compounds here described varied to a great extent, with a sigma(2)/sigma(1) selectivity ranging from 0.1 to 9. Thus, to confirm the ability of the piperazine derivative to bind to sigma(1) receptors in a different way than piperidines, we synthesized and tested a series of piperazine compounds; the comparison of their affinity with that of the corresponding piperidines strongly supports the possibility of a different binding mode. While the compounds here described are on the whole selective for sigma vs serotonin 5-HT(1A) and dopamine D(2) receptors, 9aa, 9ba and 9ab possess a remarkable affinity for both sigma and 5-HT(1A) receptors, with K(i) in the nanomolar range, and are selective with respect to D(2) receptors. They displayed also a partial agonist profile in a human 5-HT(1A) [(35)S]GTP gamma S binding assay, suggesting their potential use as atypical antipsychotic agents.


Assuntos
Receptores sigma/agonistas , Relação Estrutura-Atividade , Animais , Sítios de Ligação , Bioquímica/métodos , Células Cultivadas , Avaliação Pré-Clínica de Medicamentos , Cobaias , Humanos , Concentração Inibidora 50 , Ligantes , Piperazinas/química , Piperazinas/metabolismo , Piperazinas/farmacologia , Piperidinas/química , Piperidinas/metabolismo , Piperidinas/farmacologia , Receptor 5-HT1A de Serotonina/efeitos dos fármacos , Receptor 5-HT1A de Serotonina/genética , Receptor 5-HT1A de Serotonina/metabolismo , Receptores de Dopamina D2/efeitos dos fármacos , Receptores de Dopamina D2/genética , Receptores de Dopamina D2/metabolismo , Receptores Opioides/agonistas , Receptores Opioides/efeitos dos fármacos , Receptores Opioides/genética , Receptores sigma/efeitos dos fármacos , Receptores sigma/metabolismo , Agonistas do Receptor 5-HT1 de Serotonina , Receptor Sigma-1
4.
J Med Chem ; 45(12): 2662-5, 2002 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-12036376

RESUMO

(+)-cis-N-(4-Isothiocyanatobenzyl)-N-normetazocine (BNIT) (+)-(4) was designed and synthesized as a derivative of the potent and selective sigma(1) receptor ligand (+)-cis-N-benzyl-N-normetazocine for irreversibly blocking sigma(1) binding sites. Pretreatment of guinea pig brain membranes with BNIT (0.1, 1, and 5 microM) caused a concentration-dependent loss of binding of the selective sigma(1) ligand [(3)H]-(+)-pentazocine. Binding experiments with [(3)H]-1,3-di(2-tolyl)guanidine ([(3)H]-DTG), a ligand of sigma(1) and sigma(2) receptors, showed that pretreatment with BNIT blocked only the sigma(1) component of [(3)H]-DTG binding.


Assuntos
Ciclazocina/análogos & derivados , Ciclazocina/química , Ciclazocina/síntese química , Receptores Opioides delta/antagonistas & inibidores , Acilação , Animais , Sítios de Ligação , Encéfalo/metabolismo , Ciclazocina/farmacologia , Cobaias , Técnicas In Vitro , Pentazocina/metabolismo , Ensaio Radioligante , Receptores Opioides delta/metabolismo , Estereoisomerismo
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