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  • 1
    Electronic Resource
    Electronic Resource
    Affinity of (±)-Pindolol, (-)-Penbutolol, and (-)-Tertatolol for Pre- and Postsynaptic Serotonin 5-HT1A Receptors in Human and Rat Brain (2000)
    Oxford UK : Blackwell Science Ltd.
    Journal of neurochemistry 75 (2000), S. 0 
    Details
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: There is considerable interest in the use of drugs that selectively block presynaptic (somatodendritic) serotonin 5-HT1A receptors for the adjunctive treatment of major depressive disorder. The 5-HT1A/β-adrenoceptor ligands (±)-pindolol, (-)-tertatolol, and (-)-penbutolol are currently under clinical investigation, and knowledge of their affinity at different populations of central 5-HT1A receptors is needed. Here we have determined the affinity of these drugs for presynaptic and postsynaptic 5-HT1A receptors in postmortem human and rat brain using receptor autoradiography and the selective 5-HT1A radioligand [3H]WAY-100635. The binding of [3H]WAY-100635 was specific and saturable and showed high affinity in the rat dorsal raphe nucleus and hippocampus (KD = 1.5-1.7 nM). In competition studies, the three compounds had nanomolar affinity and produced monophasic displacement of [3H]WAY-100635 binding in all regions of both species. (-)-Penbutolol and (-)-tertatolol had similar affinity for pre-and postsynaptic 5-HT1A receptors in both rat and human brain. However, in the human, but not the rat, the affinity of (±)-pindolol in dorsal raphe nucleus (Ki = 8.9 ± 1.1 nM) was slightly but significantly higher than that in hippocampus (Ki = 14.4 ± 1.5 nM in CA1). In summary, our data show that (±)-pindolol, (-)-tertatolol, and (-)-penbutolol are all high-affinity ligands at native human and rat 5-HT1A receptors. (-)-Penbutolol and (-)-tertatolol do not discriminate between the pre- and postsynaptic 5-HT1A sites tested in either species, but (±)-pindolol showed a slightly higher affinity for the presynaptic site in human brain. Further work is needed to establish whether the latter difference is clinically relevant.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1471-4159.2000.0750755.x
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  • 2
    Electronic Resource
    Electronic Resource
    Autoradiographic distribution of [3H]sumatriptan-binding sites in post-mortem human brain (1996)
    USA/Oxford, UK : Blackwell Science Ltd
    Cephalalgia 16 (1996), S. 0 
    Details
    ISSN: 1468-2982
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: The anatomical distribution of [3H]sumatriptan-binding sites was analysed in brain tissue sections from 11 subjects. Relevant concentrations of [3H]sumatriptan-binding sites were seen in areas such as visual cortex〉locus niger〉globus pallidus〉layers IV-V of the frontal cortex〉subiculum〉entorhinal cortex〉nucleus tractus solitarius〉nucleus trigeminalis caudalis. This distribution of [3H]sumatriptan-binding sites in the human brain shows some differences when compared with that of 5HT1D receptors, confirming that, besides 5HT1D,sumatriptan also binds to 5HT1F receptor subtype. Some species differences are evident between the distribution of [3H]sumatriptan-binding sites in the human brain and that reported for guinea-pig and rat brains, emphasizing that caution is needed in extrapolating experimental data from animals to humans. Furthermore, these data help to explain some of the therapeutic actions of sumatriptan. The remarkable levels of binding found in areas such as nucleus tractus solitarius and nucleus trigeminalis caudalis suggest that in migraine attacks sumatriptan could exert its specific anti-emetic effects and, partly at least, induce analgesia by directly acting over these brain nuclei.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1468-2982.1996.1605317.x
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  • 3
    Electronic Resource
    Electronic Resource
    Selective cortical decrease of high-affinity choline uptake carrier in Alzheimer's disease: An autoradiographic study using3H-hemicholinium-3 (1994)
    Springer
    Journal of neural transmission 8 (1994), S. 161-169 
    Details
    ISSN: 1435-1463
    Keywords: Al zheimer's disease ; 3H-hemicholinium-3 ; high-affinity choline uptake
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 3H-hemicholinium-3 (3H-HC-3) binding, a marker of the presynaptic high-affinity choline uptake carrier (HACU), was measured by autoradiography in several brain regions of 17 Alzheimer's disease (AD) patients and of 11 matched controls. A significant decrease in the density of3H-HC-3 binding sites was found in entorhinal cortex, hippocampus and layers I–III of the frontal cortex. By contrast, in the caudate-putamen the number of3H-HC-3 binding sites in AD cases was comparable to that of control striata. These data concur with previous results using classical presynaptic markers and reflect the loss in the activity of HACU, and, hence, in the synthesis of acetylcholine, that selectively occurs in cortical areas of AD brains due to the degeneration of presynaptic cholinergic terminals arising from the basal forebrain. However, the relatively low mean reduction in HACU in cortical areas (−40%), together with the apparent indemnity of this marker in certain severely demented AD cases, suggest that AD dementia cannot be explained simply by the loss of presynaptic terminals originating in the basal forebrain. These data seem to be a good explanation for the poor response to cholinergic replacement in AD.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02260937
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  • 4
    Electronic Resource
    Electronic Resource
    Functional and biochemical interactions between the calcium antagonist nimodipine and sufentanil
    Amsterdam : Elsevier
    Regulatory Peptides 53 (1994), S. S17-S18 
    Details
    ISSN: 0167-0115
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Medicine
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/0167-0115(94)90219-4
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  • 5
    Electronic Resource
    Electronic Resource
    [3H]Ketanserin labels 5-HT2 receptors and α1-adrenoceptors in human and pig brain membranes (1987)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 335 (1987), S. 226-230 
    Details
    ISSN: 1432-1912
    Keywords: [3H]Ketanserin ; 5-HT2 receptors ; [125I]BE 2254 ; α1-Adrenoceptors ; Human and pig brain cortex
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1) The binding characteristics of [3H]ketanserin (a reported selective radioligand for serotonin 5-HT2 receptors) and [125I]BE 2254 (which labels selectively α1-adrenoceptors) were characterized in brain frontal cortex membranes of pig and man. 2) Saturation experiments indicated that both radioligands label apparently a homogeneous class of binding sites in human and pig fontal cortex membranes. 3) Competition experiments with [125I]BE 2254 using 17 agonists and antagonists showed monophasic and steep curves in human and pig frontal cortex membranes. The pharmacological profile of these sites is typical of α1-adrenoceptors. 4) In competition experiments with [3H]ketanserin, most of the tested compounds displayed shallow or biphasic curves. In particular, α1-adrenoceptor-selective antagonists (prazosin, WB 4101, BE 2254...) displaced with nanomolar affinity about 15 and 40% of the specific [3H]ketanserin binding in human and pig frontal cortex membranes, respectively. 5) The minor component of [3H]ketanserin binding correlated highly significantly with [125I]BE 2254 binding in both membrane preparations. 6) The major component of [3H]ketanserin binding to pig and human frontal cortex membranes correlated significantly with [3H]ketanserin binding in rat brain cortex membranes (which is essentially to 5-HT2 receptors). 7) The present data demonstrate that [3H]ketanserin in nanomolar concentrations binds significantly to α1-adrenoceptors in human and pig frontal cortex membranes; this suggests a rather limited degree of selectivity of ketanserin for 5-HT2 receptors in pig and human tissues.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00172788
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  • 6
    Electronic Resource
    Electronic Resource
    Autoradiographic mapping of 5-HT1 receptors in the guinea-pig brain with particular reference to the 5-HT1D receptor sites (1993)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 347 (1993), S. 248-256 
    Details
    ISSN: 1432-1912
    Keywords: 5-HT1 receptor distribution ; Mammalian brain ; Basal ganglia ; Hippocampus ; Species differences
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The anatomical distribution of 5-HT1 receptors in the guinea-pig brain was studied by means of in vitro quantitative autoradiography using [3H]-5-HT as ligand. The relative presence of the subtypes of the 5-HT1 binding site was investigated by adding selective concentrations of 8-OH-DPAT, (-)21009, mesulergine and 5-CT In addition, differentiation of 5-HT1D receptors was achieved by incubation of the tissues with [3H]-5-HT in the presence of 100 nmol/1 8-OH-DPAT together with 100 nmol/1 mesulergine. Areas presenting high densities of 5-HT1A receptors included the neocortex (internal layers), hippocampal formation (dentate gyrus, CA1 field), septum and raphe nuclei, while 5-HT1C sites accounted for most of the [3H]-5-HT binding to the choroid plexus. Non 5-HT1A-non 5-HT1C sites (mainly 5-HT1D and, also probably, 5-HT1E receptors) were clearly predominant in the guinea-pig brain. These sites were mainly present in the neocortex (external layers), basal ganglia, hypothalamus and midbrain (substantia nigra, superior colliculus). As previously described, sites with the properties of 5-HT1B receptors could not be clearly identified in the guinea-pig brain. The present results, in addition to providing a detailed map of the 5-HT1 receptors in the guinea-pig brain, indicate that the guinea-pig is a useful laboratory animal for the study of 5-HT1D receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00167442
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  • 7
    Electronic Resource
    Electronic Resource
    Influence of the gametogenic cycle on the biochemical composition of the ovary of the great scallop (1996)
    Springer
    Aquaculture international 4 (1996), S. 201-213 
    Details
    ISSN: 1573-143X
    Keywords: Biochemical composition ; Gametogenesis ; Great scallop (Pecten maximus) ; Lipids
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: The oogenic cycle and biochemical composition of the ovary of raft-cultured great scallop (Pecten maximus) were studied during the period April 1990–July 1991. The ovary condition index (FGI) and stereological studies showed the existence of two principal spawning periods, winter and late spring-early summer. No sexual resting period was found. Oocyte lysis was high throughout the year. Ovarian lipid levels displayed a clear seasonal pattern linked to the gametogenic cycle. Total lipid (TL, 16–21% dry weight), acylglycerol (AG, 20–65% TL) and free sterol (FS, 2.8–6.4% TL) levels were, generally, higher in the ripe ovary and a decrease coincided with spawning. Protein (59–63% dry weight), glycogen (〈3% dry weight) and phospholipid (PL, 26–35% TL) levels showed no clear seasonal trend. The TL and AG were a good index of ovarian sexual maturity. The TL % of dry weight) correlated well with the female gonad condition index (r s = 0.779, p 〈 0.001), and AG (% f TL) correlated well with the mean oocyte diameter (r s = 0.630, p 〈 0.01) and the female gonad condition index (r s = 0.443, p 〈 0.05).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00117382
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  • 8
    Electronic Resource
    Electronic Resource
    Adrenergic receptors in the cerebellum of olivopontocerebellar atrophy (1994)
    Springer
    Journal of neural transmission 96 (1994), S. 135-142 
    Details
    ISSN: 1435-1463
    Keywords: Alpha2-adrenoceptors ; autoradiography ; β-adrenoceptors ; 3H-bromoxidine ; 125I-iodocynaopindolol ; cerebellum ; olivopontocerebellar atrophy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Using autoradiographic techniques we studied the changes that in adrenergic receptors occurred in the cerebellum of two olivopontocerebellar atrophy (OPCA) patients as compared with a control group. In OPCA cerebellum the densities of total β-adrenoceptors were reduced along the cortex but increased in the white matter. Although mainly the β1 subtype was decreased along the cerebellar cortex, the increase of β-receptors over the white matter was due to a selective raise in the β2 subtype. These findings suggest a post-synaptic neuronal location for the β1 subtype and a glial location for the β2-adrenoceptor. On the other hand, alpha2-adrenoceptors were clearly reduced all along the cerebellar cortex of these OPCA brains, this probably being secondary to the loss of presynaptic adrenergic terminals arising from the locus coeruleus. These results help clarify both the subcellular location of adrenoceptors in human cerebellum and the neurochemical pathophysiology of OPCA.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01277935
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