Population genomics reveals how 5 ka of human occupancy led the Lima leaf-toed gecko (Phyllodactylus sentosus) to the brink of extinction.

Small species with high home fidelity, high ecological specialization or low vagility are particularly prone to suffer from habitat modification and fragmentation. The Lima leaf-toed gecko (Phyllodactylus sentosus) is a critically endangered Peruvian species that shelters mostly in pre-Incan archeological areas called huacas, where the original environmental conditions are maintained. We used genotyping by sequencing to understand the population genomic history of P. sentosus. We found low genetic diversity (He 0.0406-0.134 and nucleotide diversity 0.0812-0.145) and deviations of the observed heterozygosity relative to the expected heterozygosity in some populations (Fis - 0.0202 to 0.0187). In all analyses, a clear population structuring was observed that cannot be explained by isolation by distance alone. Also, low levels of historical gene flow were observed between most populations, which decreased as shown in contemporary migration rate analysis. Demographic inference suggests these populations experienced bottleneck events during the last 5 ka. These results indicate that habitat modification since pre-Incan civilizations severely affected these populations, which currently face even more drastic urbanization threats. Finally, our predictions show that this species could become extinct in a decade without further intervention, which calls for urgent conservation actions being undertaken.

Anfibios y reptiles del departamento de Ica con comentarios sobre su distribución

En este trabajo se presenta el listado actualizado de anfibios y reptiles de Ica. Las especies son comentadas, acompañadas de mapas de distribución y claves de identificación para reptiles y anfibios. Se recopiló información de registros en colecciones científicas, artículos científicos, informes de agencias gubernamentales de vida silvestre y bases de datos taxonómicas especializadas. Adicionalmente, entre los años 2019 y 2020 se realizaron evaluaciones de campo en zonas con vacíos de información. Se encontraron un total de 22 especies (anfibios 3 y reptiles 19). Los nuevos registros de reptiles para Ica incluyen la lagartija Liolaemus evaristoi y la serpiente Incaspis tachymenoides en la provincia de Chincha a 4200 y 3200 m de altitud respectivamente, la lagartija Stenocercus ornatissimus y la serpiente ciega Epictia tesselata en la provincia de Pisco a 3500 y 2800 m respectivamente. Los nuevos registros de anfibios incluyen a Pleurodema marmoratum en la provincia de Chincha (3900 m) y Telmatobius rimac en las provincias de Chincha y Palpa a 3900 y 2350 m respectivamente. La mayor riqueza y endemismos locales se encontraron en el desierto costero, mientras que, las ampliaciones de distribución y endemismos regionales se registraron en la vertiente occidental de los Andes. También, se observa que las familias Leptotyphlopidae y Viperidae, y los géneros Dicrodon, Stenocercus y Oxyrophus terminan su distribución en la vertiente occidental y la zona costera de los departamentos de Ica y Arequipa sin representantes en el extremo sur del Perú y Chile.

This paper presents the updated list of amphibians and reptiles of Ica. Species are commented, accompanied by distribution maps and identification keys for reptiles and amphibians. Information was collected from scientific collections, scientific articles, governmental wildlife agency reports, and specialized taxonomic database. Additionally, between 2019 and 2020, field surveys were carried out in areas with information gaps. A total of 22 species were found (amphibians 3 and reptiles 19). The new records of reptiles include the Liolaemus evaristoi lizard and the Incaspis tachymenoides snake from Chincha province at 4200 and 3200 m altitude respectively, the Stenocercus ornatissimus lizard and the blind snake Epictia tesselata from Pisco province at 3500 and 2800 m respectively. New amphibian records include Pleurodema marmoratum in Chincha province (3900 m) and Telmatobius rimac in Chincha and Palpa provinces at 3900 and 2350 m respectively. The greatest richness and local endemism were found in the coastal desert, while the expansion of distribution and regional endemism were recorded on the western slope of the Andes. Also, it is observed that the families Leptotyphlopidae and Viperidae, and the genera Dicrodon, Stenocercus and Oxyrophus are finishing their distribution in the western slope and the coastal zone of the departments of Ica and Arequipa without representatives in the extreme south of Peru and Chile.

Ampliación de la distribución geográfica y estado de conservación de Ctenoblepharys adspersa (Tschudi, 1845)

Ampliamos la distribución geográfica de Ctenoblepharys adspersa (Liolaemidae), una especie de saurio endémico y amenazado del desierto peruano. Nuestro nuevo registro extiende la distribucion de esta especie en 60 km (línea recta) de la localidad más oriental previamente conocida, la Reserva Nacional de Paracas. Registramos dos tipos de hábitat nuevos para C. adspersa al interior de las estribaciones andinas e identificamos las plantas nativas asociadas a sus hábitats. Además, revisamos el estado de conservación de esta especie y los desafíos que implican su conservación, resaltando que la mayoría de las poblaciones son vulnerables a los impactos en su hábitat producto del desarrollo de infraestructura urbana y/o agrícola.

We extend the geographical distribution of Ctenoblepharys adspersa (Liolaemidae) an endemic and threatened lizard species from the Peruvian desert. Our new record extends the known species distribution ca. 60 km (straight line) east-southeastern from the eastemost record at Paracas National Reserve. We recorded two new type of habitat for C. adspersa that reach to the Pacific foothills and identified the native plants associated to its habitats. Moreover, we review the conservation status and the challenges that facing it, highlighted that most of its populations are vulnerable to the impacts on their habitat caused by the development of urban and agricultural infrastructure.

Ámbito de Hogar de la lagartija de las lomas Microlophus tigris (Sauria: Tropiduridae) en las Lomas de Carabayllo, Lima - Perú / Home Range of Lomas Lizard Microlophus tigris (Sauria: Tropiduridae) in Carabayllo Lomas, Lima - Peru

El ámbito de hogar o "home range", es el área donde un individuo encuentra todos los recursos para su supervivencia, por ende su estudio es fundamental para conocer su ecología y estado de conservación. La lagartija de las Lomas, Microlophus tigris, es una especie endémica de la costa central del Perú, cuyo ámbito de hogar no ha sido estudiado. Para estudiar el uso del espacio de M. tigris se evaluó el ámbito de hogar de 15 individuos (9 machos y 6 hembras) durante la época no reproductiva en las Lomas de Carabayllo, Lima, Perú. Se empleó el método del Mínimo Polígono Convexo para estimar el área del ámbito de hogar. Los machos fueron significativamente más grandes y pesados que las hembras. No obstante, no hubo diferencias significativas entre el ámbito de hogar de los machos y hembras debido a la variabilidad del ámbito de hogar de los machos. El tamaño del ámbito de hogar de las lagartijas evaluadas no estuvo relacionado con su tamaño corporal (Longitud hocico-cloaca) ni con su peso. La ausencia de relación entre el ámbito de hogar y las variables analizadas sugiere que el tamaño del ámbito de hogar de estos reptiles, durante la época no reproductiva, respondería a otros parámetros como la abundancia de recursos, condiciones climáticas, entre otros. La baja superposición del ámbito de hogar intra e intergéneros, indicaría una evidencia indirecta de comportamiento territorial. A partir de nuestros datos y antecedentes en otras especies de saurios, consideramos que puede haber variaciones en el uso del espacio durante otras épocas del año, por lo tanto se necesitan evaluaciones complementarias a lo largo del año para observar los otros factores que determinan el tamaño del ámbito de hogar de M. tigris

The home range is the area where an individual finds the resources for its survival; therefore, the home range studies of organisms are fundamental to know their ecology and conservation status. The Loma's lizard, Microlophus tigris is an endemic species of Peruvian central coast, whose home range has not been studied. We used the Minimum Convex Polygon method on 15 individuals (9 males and 6 females) to estimate the home range of M. tigris during the non-breeding season in Lomas de Carabayllo, Lima, Peru. We found males were significantly larger and heavier than females. However, there were no significant differences between male and female home ranges due to high variability in males. The home range size of the evaluated lizards was not related to their body size (snout vent-length) or their weight. The lack of relation between home range and the analyzed variables suggests that the home range size of M. tigris, during the non-breeding season, may be related to other parameters such as resource availability or climatic conditions. The low home range overlap between and among sexes, indirectly indicates there is territorial behavior. According to our data and natural history information of other species of lizards, we believe there may be variation in the spatial use during other seasons. Therefore, it is necessary complementary evaluations to observe other relevant factors that define home range of M. tigris

Obtención de queso crema con propiedades funcionales suplementado con sólidos de lactosuero e inoculado con Lactobacillus casei

En la actualidad la industria alimentaria está enfocada principalmente en la diversificación de los productos probióticos debido a los efectos beneficiosos que estos proporcionan a la salud de los consumidores. El objetivo del siguiente trabajo de investigación fue elaborar un queso crema suplementado con sólidos de lactosuero e inoculado con Lactobacillus casei. Para lo cual se realizaron análisis fisicoquímicos al lactosuero y a la leche cruda, así como al queso crema, además se evaluó parámetros microbiológicos al producto final con el fin de estimar la calidad del mismo. Los resultados indicaron que es posible obtener un queso crema con calidad óptima ya que se obtuvieron resultados de proteína y grasa comparables con el producto comercial. Igualmente es importante destacar que Lactobacillus casei se conservó viable durante 15 días a las diferentes diluciones evaluadas, 10-4, 10-5 y 10-6, con valores de UFC de 1.79E+06, 1.35E+07 y 6.80E+07, respectivamente. El queso crema mantuvo calidad microbiológica debido a que no se apreció crecimiento de microorganismos indeseables.

The food industry's current focus lies mainly on diversifying probiotic products due to their beneficial effects on consumers' health. This research was thus aimed at producing a cream cheese supplemented with whey solids and inoculated with Lactobacillus casei. Whey and fresh milk's physical-chemical properties were thus analysed, as well as those of cream cheese; the final product's microbiological parameters were also evaluated for estimating quality. The results indicated that high-quality cream cheese can be obtained since the results regarding protein and fat were comparable with those of commercial products. It is worth stressing that Lactobacillus casei remained viable for 15 days at the different dilutions evaluated here: 10-4 (1.79E+06 CFU), 10-5 (1.35E+07 CFU) and 10-6 (6.80E+07 CFU). The cream cheese maintained its microbiological quality as the growth of undesirable microorganisms was not observed.

Atualmente, a indústria de alimentos é voltada principalmente para a diversificação dos efeitos probióticos devido aos benefícios que eles proporcionam para a saúde dos consumidores. O objetivo desta pesquisa foi desenvolver um soro de leite creme de queijo suplementados com Lactobacillus casei. análise físico-química do soro e do leite e queijo creme em bruto foram realizados também parâmetros microbiológicos avaliados no produto final, a fim de estimar a qualidade do queijo. Os resultados indicaram que é possível obter um queijo creme com resultados de qualidade óptima protiena como gordura e comparável com o produto comercial foram obtidos. É também importante notar que o Lactobacillus casei foi mantida viável durante 15 dias para as diferentes diluições avaliadas, 10-4 10-6 10-5y UFC valores 1.79E + 06 1.35E + 07 6.80E + 07 e, respectivamente. Queijo creme qualidade microbiológica mantida porque nenhum crescimento de microorganismos indesejáveis apreciado.

Dieta de la lagartija de los gramadales Microlophus thoracicus icae en el valle del río Ica, Perú

Se evaluó la dieta de la lagartija de los gramadales Microlophus thoracicus icae en tres localidades del Valle del río Ica, Perú. La dieta de este saurio se caracterizó por un importante consumo de material vegetal, principalmente foliolos del árbol Prosopis spp., e invertebrados, especialmente insectos como hormigas y larvas de insectos. No se registraron relaciones significativas entre el tamaño corporal de los individuos y el número total de presas consumidos, ni el volumen total consumido. Los juveniles, hembras y machos de M. t. icae no presentaron diferencias significativas en el número de hormigas o larvas de insectos consumidos. Tampoco se registraron diferencias significativas en la proporción de material vegetal consumido por juveniles, hembras y machos. Sin embargo, el volumen de material vegetal consumido fue mayor para machos y hembras, comparado con juveniles. No se observan diferencias evidentes entre las dietas de juveniles, hembras y machos en el análisis multivariado. La amplitud del nicho trófico para M. t. icae fue de Bij = 6.97. El consumo de material vegetal e invertebrados es importante para juveniles y adultos de M. t. icae, por lo tanto, no se observa una marcada variación etaria en la dieta de los individuos evaluados. Esta especie de saurio presentaría una gran plasticidad en su dieta (omnívora) influenciada principalmente por la variación local de la oferta de los recursos alimenticios. Las posibles consecuencias del consumo de una dieta tan variada podrían incluir características particulares en sus endoparásitos, estrategias y eficiencia de forrajeo, termorregulación, morfología, entre otros.

The diet of grass lizard, Microlophus thoracicus icae, was evaluated in three localities of the Ica River Valley, Peru. The dietary pattern was characterized by high consumption of vegetable material, mainly Prosopis spp. leaves, and invertebrates as ants and insect larvae. No significant relationships were found between body size, number of prey eaten or volume consumed. The juvenile, male and female M. t. icae not showed significant differences regarding number of ants or insect larvae consumed, neither on the proportion consumed of plant material. However, total volume of plant material was different between males and females, compared to juveniles. Multivariate analysis showed no evident difference in the diets of juveniles, males and females. Trophic niche amplitude for M. t. icae was Bij = 6.97. The consumption of plant material and invertebrates is important for both juvenile and adult iguanas, therefore; no clear age difference in diet was observed in the individuals studied. This species would present great diet plasticity (omnivory) influenced by the local variation of food resources. Possible consequences of a varied diet may include particular characteristics of its parasites, foraging strategies and efficiency, thermoregulation, morphology, among others.

Reptiles terrestres de la isla San Lorenzo, Lima, Perú

Se reportan cuatro especies de reptiles terrestres, un gecónido (Phyllodactlus cf. microphyllus), dos lagartijas (Microlophus peruvianus y M. tigris) y una culebra (Pseudalsophis elegans) para la isla San Lorenzo, departamento de Lima, Perú. La lagartija de las lomas M. tigris y la culebra P. elegans son reportadas por primera vez para las islas del mar peruano. La presencia de lomas de herbáceas y la considerable extensión de la Isla San Lorenzo explicarían la considerablemente alta riqueza de especies de reptiles terrestres en esta isla.

We report four species of terrestrial reptiles, a geckonid (Phyllodactlus cf. microphyllus), two lizards (Microlophus peruvianus and M. tigris) and one snake (Pseudalsophis elegans) from San Lorenzo island, Departament of Lima, Peru. Herein, we report the first record of “Lomas lizard” M. tigris and the snake P. elegans in Peruvian islands. The presence of Lomas herbaceous and the considerable extent of San Lorenzo island can explain the relatively high species richness of terrestrial reptiles on the island.

Obesidad: Influencia de la publicidad alimentaria y suplementos dietéticos en Venezuela / Obesity: food advertising influence and dietary suplements in Venezuela

La obesidad es considerada como un problema de salud pública a nivel mundial y uno de los mayores retos para los gobiernos. En Venezuela, el “Estudio de Sobrepeso y Obesidad” realizado por el Instituto Nacional de Nutrición (INN), revela el crecimiento de esta enfermedad crónica no transmisible, que a su vez, genera un número considerable de otras patologías. La etiología de la obesidad es multifactorial, pero inicialmente se pueden dividir en factores endógenos (genéticos) y exógenos (sociales, políticos, culturales y económicos); estos últimos son los más relevantes, ya que esta enfermedad ha dejado de ser un tema netamente biológico y se ha convertido en un tema social. En las últimas décadas se ha observado una marcada tendencia donde la alimentación tradicional es sustituida por una dieta hipercalórica, lo cual es incoherente con el hecho de que la población se encuentra cada día más obsesionada con la delgadez, y en los esfuerzos para alcanzarla, optan por el consumo de suplementos dietéticos de venta libre, que prometen eliminar grasa sin hacer dieta ni ejercicios. En medio de este ritmo de vida dicotómico, la industria publicitaria saca provecho de esta situación, promocionando estilos de vida poco saludables e incompatibles con el vivir bien. Es por esto que se hace necesaria la intervención inmediata del Estado a través del diseño y ejecución de políticas avocadas a disminuir el avance epidemiológico de esta enfermedad, y regular los elementos que la propician y a la vez se benefician de ella.

Obesity is considered as a public health issue worldwide and one of the biggest challenges for governments. In Venezuela, the National Institute of Nutrition (NIN) is conducting the “Obesity and Overweight” study, which reveals that this chronicle non transmissible disease is increasing and that it is the cause of a great amount of other pathologies. The obesity aetiology is multifactorial, among the main factors we found endogenous factors (genetic) and exogenous factors (social, political, and economic); the last ones are the most relevant because this illness is no longer a biological issue but it has become a social matter. In the last decades, we have observed a strong trend of traditional feeding being substituted by a high-calorie diet, which is incoherent with the fact that people is currently obsessed with thinness; in order to be thin they decide to take dietetic supplements that are sold without any regulation, these kind of products promise to eliminate fat without going on a diet or doing exercises. In nowadays dichotomist way of life, advertising industry makes advantage of that promoting really unhealthy life’s stiles which are incompatible with well living. This is the reason why it is necessary the immediate intervention of State through the design and execution of politics advocated to the decrease of the epidemiologic advance of this disease, and to the regulation of factors that launch it and benefit from it.

Análisis de los registros de presión arterial en recién nacidos pretérminos en consultorio de control ambulatorio / Analysis of records of blood pressure in preterm infants in an outpatient clinic control

El registro de PA en controles ambulatorios de los niños nacidos pretérminos no es una práctica habitual. Los objetivos de este estudio fueron: Evaluar PA y prevalencia de HTA de RNPT en control ambulatorio. Asociar HTA a factores de riesgo y patologías perinatales. POBLACIÓN. RNPT < 36 semanas (sem) dados de alta de UTIN y atendidos en consultorio ambulatorio. Período agosto 2008 a febrero 2009. Las variables estudiadas fueron edad gestacional, edad actual corregida, medidas antropométricas al nacimiento y al momento del registro: peso, talla. Patologías en UTIN. Se midió PA con tensiómetro oscilométrico manual con auscultación y palpación del pulso. Se siguió técnica y definición de PA, pre HTA e HTA 1 Y 2 de la 4a Task Force. Diseño descriptivo de corte transversal. Análisis estadístico simple y de asociación. RESULTADOS: 36 RNPT<36 s fueron estudiados, 57 por ciento de sexo femenino. Los promedios observados al nacer fueron; EG de 31.3 s IC 95 por ciento (30;32), PN 1533 gr IC95 por ciento (1397;1668), TN 40 cm (38.8; 41.3). Al momento del registro, EAC 11.8 m IC 95 por ciento (8.9;14.7), PA 8594 gr IC95 por ciento (7763; 9424). 19 por ciento con BPEG; 16 por ciento con TBEG; 3 po ciento TAEG. Se registró PAS a 32 niños (86,5 por ciento) , 6 por ciento fueron Pre-HTAS (P90-95); 6 por ciento HTAS grado I y 6 por ciento HTAS grado 11. En 50 por ciento se registró PAD, 6 por ciento pre HTAD; 25 por ciento con HTAD 1; 6% con HTAD 2. 27 niños tuvieron algún antecedente patológico perinatal, CAU 19 por ciento, 57 por ciento EMH, 51 por ciento sepsis, 41 por ciento ARM, 14 por ciento HIV, esta última se asoció significativamente con HTA (p=0.01). DISCUSIÓN Y CONCLUSIONES: En los más pequeños fue difícil registrar PA con este método. Encontramos mayor prevalencia de HTA en este grupo y asociación de HTA con HIV. El seguimiento será fundamental...

The registration of BP (Blood Pressure) in ambulatory monitoring of children born pre-term is not common practice. The objectives of this study were: to evaluate BP and Hypertension of newborns in outpatient control, associate Hypertension risk factors and perinatal pathology. POPULATION: pre term newborns of 36 weeks discharged from NICU and treated at an outpatient clinic. PERIOD: August 2008 to February 2009. The variables studied were: gestational age, corrected current age, anthropometric measurements at birth and the time of recording: weight, height. Pathologies in NICU. BP (Blood Pressure) was measured with an oscillometric blood pressure monitor with manual auscultation and pulse palpation. It was followed by technique and definition of BP, pre Hipertension, e Hipertension 1 y 2 of the fourth Task Force. Cross sectional descriptive design. Simple and association statistical analysis. RESULTS: 36 newbons 36 weeks were studied, 57 per cent female. The averages observed at birth were: GA (Gestational Age) 31.3 CI (Confidence Interval) 95 per cent (30:32), WB (Weight at Birth) 1533 gr 95 per cent (1397, 1668), HB (Height at Birth) 40 cm (38.8; 41.3). At the time of registration: CCA (Corrected Current Age) 118 m 95 per cent (8.9; 14.7), 8594 BP (Blood Pressure) 95 per cent gr (7763, 9424). 19 per cent in LWGA (Low Weight for Gestational Age), LHGA (Low Height for Gestational Age) 16 per cent, RHGA (Right Height for Gestational Age) 3 per cent. SBP (Systolic Blood Pressure) was recorded in 32 children (86,5 per cent), 6 per cent were pre-HBPs (P 90-95), 6 per cent HBP grade 1, and 6 per cent were HBP grade II...

Cutaneous miliary resistant tuberculosis in a patient infected with human immunodeficiency virus: case report and literature review.

We report the case of a patient infected with human immunodeficiency virus who presented with fever and a disseminated papulous eruption, diagnosed as cutaneous miliary tuberculosis. The diagnosis was made by histological examination of a skin biopsy, which showed numerous acid-fast bacilli. A culture grown from a skin biopsy isolated a resistant Mycobacterium tuberculosis strain. The papules disappeared within a few days after starting treatment with pyrazinamide, isoniazid and moxifloxacin.

Ecología de la comunidad de saurios diurnos de la Reserva Nacional de Paracas, Ica, Perú

En el presente trabajo estudiamos algunos aspectos de la ecología de la comunidad de saurios diurnos de la Reserva Nacional de Paracas (RNP) desde abril a setiembre de 1999. Analizamos la distribución espacial, el uso del hábitat (nicho espacial), patrones de actividad (nicho temporal) y la dieta (nicho trófico) de estos reptiles, con el objetivo de identificar las principales diferencias que permitirían la división en el uso de los recursos. Estas especies mostraron preferencias por algunos hábitats, a excepción de Microlophus peruvianus, la lagartija de los arenales M. theresiae y la lagartija de los gramadales M. thoracius icae. Las especies mostraron preferencias por algunos hábitats, a excepción de Microlophus peruvianus que estuvo presente en todos los hábitats. La actividad de los saurios se concentraron al medio día, a excepción de C. adspersa. La dieta de estos saurios esta compuesta principalmente por insectos. Los saurios diurnos en la RNP presentan diferencias en el nicho trófico, espacial y/o temporal que posibilitarían su coexistencia en simpatría.

In present paper we study some ecological aspects of the diurnal saurian community of National Reserve of Paracas (RNP) since April to September 1999.". The spatial distribution, habitat uses (spatial niche), activities patterns (temporal niche) and the diet (trophic niche) of these reptiles were analyzed with the objective of identifying the main differences that will allow a division in the use of the resources. Ctenoblepharis adspersa (bigheaded lizard), Microlophus peruvianus (beach lizard), M. theresiae (dune lizard) and M. thoracius icae (grass lizard) were the species studied. Each lizard showed preference for some particular habitat, to exception of M. peruvianus that was present in all the habitats. The activity was concentrated to the half-day, to exception of C. adspersa. The diets were mainly insects. Differences in trophic, temporal and spatial niche were observed and these would facilitate the coexistence in sympatry of species lizards.

Rituximab en artritis reumatoide / Use of rituximab in rheumatoid arthritis

Rituximab, a human/mouse chimeric anti-CD20 antibody, has become part of rheumatoid arthritis therapy . Rituximab induces a rapid depletion of normal CD20 expressing B cells in the peripheral blood, and levels remain low or undetectable for 2-6 months before returning to pre-treatment levels. T cells are unaffected by rituximab and, consequently, opportunistic infections rarely occur in association with rituximab therapy.

Synthesis of 1-amino-6,7,8,8a-tetrahydroacenaphthene and its effect on the inhibition of the MAO-enzyme at the brain cortex and liver level.

(+/-)-1-Amino-6,7,8,8a-tetrahydroacenaphthene was synthesized and evaluated as a novel drug acting on the dopaminergic system. It was shown that the new compound displays activity as MAO inhibitor.

Synthesis and theoretical study of 2-amino-2,3,3a,4,5,6-hexahydro-1H-phenalene and its biological evaluation on central dopaminergic system.

Compound 2 considered as a rigid non-hydroxylated 2-amino tetralin was synthesized and biologically evaluated. Central administration of compound 2 (50 microg or 100 microg/10 microl) induced a reduction in urinary sodium and potassium excretion at 3 and 6 h of urine collection. We speculate that compound 2 may be acting as a dopamine receptor antagonist.

N-aralkyl substitution of 2-aminoindans. Synthesis and their inotropic and chronotropic activity in isolated guinea pig atria.

Amino substitution of rigid forms of dopamine 4,5-dihydroxy-2-aminoindan and 5,6-dihydroxy-2-aminoindan with aralkyl functionalities were carried out to investigate the role of such structural modifications upon cardiac inotropic-chronotropic activity. Compounds synthesized demonstrated a modest inotropic selectivity, while one of them, described as 5,6-dihydroxy-N-[2-(4-hydroxyphenyl)-1-methylethyl]-2-aminoindan hydrobromide 17, showed a marked inotropic action on isolated heart tissue.

Synthesis of (+/-)-1-amino-6,7,8,8a-tetrahydro acenaphthene with possible central dopaminergic activity.

We describe the non stereoselective synthesis of (+/-)-1-amino-6,7,8,8a-tetrahydroacenaphthene (14), a novel compound that belongs to the acetanaphtene group, that is presented as a rigid non hydroxylated 2-aminoindan which has a structural disposition of a dopaminergic pharmacophore that possess a phenylethylamine fragment. Intracerebroventricular administration of this compound induces an increase in urinary volume and sodium excretion in conscious rats. The renal actions of 14 were blocked by haloperidol pretreatment, suggesting that 14 acts centrally through a dopaminergic mechanism.

1-(Aminomethyl)-6,7-dihydroxytetralin derivatives: synthesis and assessment of dopamine-like effects.

The title compounds were designed as flexible congeners of trans-octahydrobenz[h]isoquinoline, in which the dopamine moiety can exist in the alpha conformation. Extremely low dopamine-like effects in the title series in the cat cardioaccelerator nerve assay paralleled low activity in the trans-octahydrobenz[h]isoquinoline compounds and was consistent with a prior proposal of the presence of a bulky region on the dopamine receptor(s).

N-Alkyl derivatives of (+/-)-alpha-methyldopamine.

A series of N-alkylated alpha-methyldopamine derivatives has been prepared for comparison of their biological effects with those of semirigid dopamine congeners derived from 2-aminotetralin systems. All of the alpha-methyldopamine derivatives were inert as dopaminergic agonists in a variety of animal assays, both centrally and peripherally, although certain compounds produced powerful and prolonged locomotor hyperactivity on intra-accumbens injection in mice, by indirect mechanism(s). A rationalization, based upon conformational analysis, is presented for the lack of direct dopaminergic agonist activity of alpha-methyldopamine derivatives.