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Biomedical subjects

R Gough

Publications and source records attributed to R Gough.

6 recordsLinked to original sources
PubMed2001

beta-carboline binding to imidazoline receptors.

A series of beta-carbolines were prepared and their affinities for imidazoline (I(1) and I(2)) sites evaluated. Selected compounds were also examined at alpha(2)-adrenoceptors. Some of the beta-carbolines were found to bind with high affinity to I(2)-sites and this affinity was dependent on both the planarity of the molecule and the presence of the aryl ring substituents. Good I(1)-affinity was observed with two of the compounds but none of the tested compounds bound to alpha(2)-adrenoceptors. The hallucinogenic properties of beta-carbolines have been linked to activity at 5-HT receptors, in particular 5-HT(2), however, it is apparent from this study that many of these compounds display substantially higher affinity for the imidazoline sites. This finding, and those showing modulation of some behavioural effects of morphine by I(2)-ligands, suggests that imidazoline sites may be interesting new targets in drug abuse research.

Animals↗
PubMed2001

3-Hydroxyisobutyric aciduria: phenotypic heterogeneity within a single family.

3-Hydroxyisobutyric aciduria is a rare biochemical finding associated with a variable clinical phenotype in the literature. We report two siblings excreting abnormal levels of this metabolite from a consanguineous family who manifested distinct phenotypic variation. We speculate as to whether this biochemical anomaly may simply be an incidental finding and suggest that pre-natal counselling on the basis of metabolite identification may be unwarranted.

Child↗
PubMed1999

Novel selective compounds for the investigation of imidazoline receptors.

Over several years our group has sought to synthesize and identify selective ligands for imidazoline (I) receptors, in particular the I2 binding site. As a consequence, [3H]2-(2-benzofuranyl)-2-imidazoline (2BFI) has proved extremely useful for binding and autoradiographic studies. More recently we have synthesized a BU series of compounds and examined these for their affinities for both I1 and I2 binding sites. BU224 (2-(4,5-dihydroimidaz-2-yl)-quinoline) shows high affinity for I2 receptors with a Ki of 2.1 nM. BU226 (2-(4,5-dihydroimidaz-2-yl)-isoquinoline) demonstrated slightly higher affinity (Ki 1.4 nM) for I2 receptors, but overall BU224 displayed greater selectivity for I2 over I1 receptors (832-fold) than BU226 (380-fold). Both compounds showed low (microM) affinity for alpha 2-adrenoceptors. Given BU224's ability to cross the blood brain barrier, we predict that its in vivo effects are likely to be mediated via I2 receptors. Brain dialysis revealed BU224 to dose dependently (0-20 mg/kg i.p.) elevate basal noradrenaline in rat frontal cortex and basal dopamine in striatum. In a rat model of opiate withdrawal, behavioral studies showed that BU224 (10 mg/kg, s.c.) was able to reduce acute weight loss and diarrhea, but not the number of wet dog shakes associated with the withdrawal syndrome.

Animals↗
PubMed1976

An international haematological survey.

Haematological surveys of adult population samples were conducted simultaneously in 12 countries, all but one of which are in Europe. Haematological estimations on samples from nine of the countries were made in one central laboratory. Differences between countries in the mean levels of haemoglobin (and haematocrit and red cell count) were found to be relatively small, and the prevalence of levels below the arbitrary WHO levels for anaemia were, on the whole, low. In males, the evidence suggests a fall in haemoglobin level throughout adult life, which increases slightly in advanced age. In females, there is no evidence of any important relationship between age and haemoglobin level.

Adolescent↗