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Introducción. La pandemia de COVID-19 replanteó la forma de atención en los sistemas de salud, afectando todas aquellas patologías no relacionadas con infecciones respiratorias, como la apendicitis aguda. El miedo al contagio por SARS-CoV-2 y las medidas restrictivas a la movilidad pudieron aumentar el tiempo desde el inicio de los síntomas hasta la consulta al servicio de urgencias, derivando en complicaciones intra y posoperatorias. Métodos. Estudio observacional descriptivo de corte trasversal y retrospectivo, donde se incluyeron todos los pacientes diagnosticados con apendicitis aguda llevados a apendicectomía, que fueron divididos en dos grupos, considerados pre-pandemia, desde el 1° de septiembre de 2018 al 15 de marzo de 2020, y pandemia, desde el 16 de marzo de 2020 al 30 de septiembre de 2021. Resultados. Fueron identificados 1000 pacientes, distribuidos en 501 pacientes en el grupo pre-pandemia y 499 en el grupo pandemia. El promedio de tiempo de consulta desde el momento de inicio de síntomas hasta consulta fue de 43 horas en el grupo pre-pandemia y de casi 45 horas en el grupo pandemia. Discusión. A pesar de las restricciones por la enfermedad causada por el nuevo coronavirus y el miedo que puede existir por el contagio, en nuestro centro no se evidenció un cambio en el manejo y presentación de los pacientes diagnosticados con apendicitis aguda.

Objetivo: evaluar la prevalencia de yodo deficiencia y de bocio en mujeres indígenas gestantes de cinco áreas no metropolitanas en Colombia. Materiales y métodos: estudio de corte transversal descriptivo. Se incluyeron mujeres embarazadas de cualquier edad gestacional sin condiciones patológicas del embarazo, atendidas en los centros de salud comunitarios o en sus residencias. Se excluyeron aquellas con comorbilidades presentes al momento del embarazo y también a quienes recibían suplementos con yodo. Muestreo aleatorio simple. Se midieron las características sociodemográficas y obstétricas, la concentración de yodo en orina y la presencia de bocio de acuerdo a la metodología de la Organización Mundial de la Salud. Se realizó un análisis descriptivo. Resultados: 189 gestantes indígenas fueron candidatas a ingresar al estudio, de las cuales 2 no aceptaron participar y 62 tenían criterios de exclusión, finalmente se analizaron 125. La concentración urinaria de yodo tuvo una mediana de 184.4 μg/L (rango 12.0-390.0). Un total de 42 gestantes (33.6%) tenían yodo deficiencia (< 100 μg/L) y se evidenció bocio (grado 1-2) en 43 (34.4%). No se evidencia bocio grados 3 o 4. Conclusiones: embarazadas indígenas residentes en áreas no metropolitanas evidenciaron alta prevalencia de bocio y yodo deficiencia. Se requiere evaluar los efectos materno-perinatales e implementar intervenciones nutricionales.

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Inour overall goal to develop multifunctional dopamine D2/D3agonist drugs for the treatment of Parkinson’sdisease (PD), we previously synthesized potent D3preferringagonist D-264 (1a), which exhibited neuroprotective propertiesin two animal models of PD. To enhance the in vivo efficacy of 1a, a structure–activity relationship study was carriedout. Competitive binding and [35S]GTPγS functionalassays identified compound (−)-9bas one of thelead molecules with preferential D3agonist activity (EC50(GTPγS); D3= 0.10 nM; D2/D3(EC50): 159). Compounds (−)-9band (−)-8bexhibited high in vivo activity intwo PD animal models, reserpinized and 6-hydroxydopamine (OHDA)-inducedunilateral lesioned rats. On the other hand, 1afailedto show any in vivo activity in these models unless the compound wasdissolved in 5–10% beta-hydroxy propyl cyclodextrin solution.Lead compounds exhibited appreciable radical scavenging activity.In vitro experiments with dopaminergic MN9D cells indicated neuroprotectionby both 1aand (−)-9bfrom toxicityof MPP+. [ABSTRACT FROM AUTHOR]

Abstract: Here we report a structure–activity relationship (SAR) study of analogues of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol. Our SAR is focused on introduction of various substitutions in the piperazine ring of the hybrid template. The goal behind this study is to delineate the nature of the binding pocket for N-aryl substitution in the piperazine ring by observing the effect of various hydrophobic and other heteroaromatic substitutions on binding affinity (K i), as measured with tritiated spiperone and HEK-293 cells expressing either D2 or D3 receptors. Functional activity of selected compounds was assessed with the GTPγS binding assay. Compound 8d was the most selective for the D3 receptor in the spiperone binding assay. An interesting similarity in binding affinity was observed between isoquinoline derivative D-301 and the 2-substituted pyridine derivative 8d, suggesting the importance of relative spatial relationships between the N-atom of the ligand and the molecular determinants of the binding pocket in D2/D3 receptors. Functional activity assays demonstrated high potency and selectivity of (+)-8a and (−)-28b (D2/D3 (ratio of EC50): 105 and 202, respectively) for the D3 receptor and both compounds were more selective compared to the reference drug ropinirole (D2/D3 (ratio of EC50): 29.5). [ABSTRACT FROM AUTHOR]

Abstract: In receptor binding assays with ultra-high-affinity radioligands, it is difficult, in practice, to adhere the golden rule that the receptor concentration in the assay should be substantially (at least 10-fold) lower than the dissociation constant (K d) of the radioligand and inhibition constant (K i) of compound. Especially for low specific activity radioligands (usually tritiated ligands of a couple of TBq/mmol), routinely applied in concentrations at around or below the K d, the use of extremely small amounts of receptor protein per assay will result in low levels of bound radioactivity; the alternative use of larger assay volumes will make it difficult to apply 96-well filtration devices. For assessing the inhibition constant (K i) of competitive inhibitors under conditions violating the above golden rule, equations are available incorporating both [receptor] and [ligand] versus K d; however, their application requires precise knowledge of [receptor] or initial bound/free [radioligand] ratio. In this study, we present the theoretical basis for determining the K i for a competitive inhibitor in a new protocol at high [protein] and high [radioligand] with the simple Cheng–Prusoff correction without the need to correct for [receptor] or initial bound/free [radioligand] ratio. In addition, we present results on the binding of the ultra-high-affinity ligand [3H]spiperone to dopamine D2 and D3 receptors validating the K i values calculated with the new protocol for competitive inhibitors as compared with those calculated with the most comprehensive equation available to date, that of . Binding was measured at varying [radioligand] and [receptor], test compounds (including (−)5-OH-DPAT, (±)7-OH-DPAT, and ropinirole) were run with varying [receptor], and simulations were done at vastly varying [radioligand] for inhibitors with vastly different K is. The modified high [radioligand] protocol presented here removes a major hindrance in the proper execution of binding assays with ultra-high-affinity tritiated ligands with K d values in the sub-nanomolar range, allowing the use of 96-well plates with small volumes of 100–200μl per binding assay. [Copyright &y& Elsevier]