19,875 research outputs found
The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT3 receptors.
Scopolamine is a high affinity muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. 5-HT3 receptor antagonists are used for the same purpose and are structurally related to scopolamine. To examine whether 5-HT3 receptors are affected by scopolamine we examined the effects of this drug on the electrophysiological and ligand binding properties of 5-HT3A receptors expressed in Xenopus oocytes and HEK293 cells, respectively. 5-HT3 receptor-responses were reversibly inhibited by scopolamine with an IC50 of 2.09 μM. Competitive antagonism was shown by Schild plot (pA2 = 5.02) and by competition with the 5-HT3 receptor antagonists [(3)H]granisetron (Ki = 6.76 μM) and G-FL (Ki = 4.90 μM). The related molecule, atropine, similarly inhibited 5-HT evoked responses in oocytes with an IC50 of 1.74 μM, and competed with G-FL with a Ki of 7.94 μM. The reverse experiment revealed that granisetron also competitively bound to muscarinic receptors (Ki = 6.5 μM). In behavioural studies scopolamine is used to block muscarinic receptors and induce a cognitive deficit, and centrally administered concentrations can exceed the IC50 values found here. It is therefore possible that 5-HT3 receptors are also inhibited. Studies that utilise higher concentrations of scopolamine should be mindful of these potential off-target effects.Our thanks are given to John Peters (University of Dundee) for the 5-HT3A subunit. ML thanks the Swiss National Science Foundation for financial support (SNSF- professorship PP00P2_123536 and PP00P2_146321). AJT thanks the British Heart Foundation for financial support (PG/13/39/30293).This is final version of the article. It first appeared from Elsevier via http://dx.doi.org/10.1016/j.neuropharm.2016.04.02
Time-resolved photoelectron imaging of excited state relaxation dynamics in phenol, catechol, resorcinol and hydroquinone
Time-resolved photoelectron imaging was used to investigate the dynamical evolution of the initially prepared S1 (\u3c0\u3c0*) excited state of phenol (hydroxybenzene), catechol (1,2-dihydroxybenzene), resorcinol (1,3-dihydroxybenzene), and hydroquinone (1,4-dihydroxybenzene) following excitation at 267 nm. Our analysis was supported by ab initio calculations at the coupled-cluster and CASSCF levels of theory. In all cases, we observe rapid (<1 ps) intramolecular vibrational redistribution on the S1potential surface. In catechol, the overall S1 state lifetime was observed to be 12.1 ps, which is 1\u20132 orders of magnitude shorter than in the other three molecules studied. This may be attributed to differences in the H atom tunnelling rate under the barrier formed by a conical intersection between the S1 state and the close lying S2 (\u3c0\u3c3*) state, which is dissociative along the O\u2013H stretching coordinate. Further evidence of this S1/S2 interaction is also seen in the time-dependent anisotropy of the photoelectron angular distributions we have observed. Our data analysis was assisted by a matrix inversion method for processing photoelectron images that is significantly faster than most other previously reported approaches and is extremely quick and easy to implement.Peer reviewed: YesNRC publication: Ye
How does breakup influence the total fusion of Li at the Coulomb barrier?
Total (complete + incomplete) fusion excitation functions of Li on
Co and Bi targets around the Coulomb barrier are obtained using
a new continuum discretized coupled channel (CDCC) method of calculating
fusion. The relative importance of breakup and bound-state structure effects on
total fusion is particularly investigated. The effect of breakup on fusion can
be observed in the total fusion excitation function. The breakup enhances the
total fusion at energies just around the barrier, whereas it hardly affects the
total fusion at energies well above the barrier. The difference between the
experimental total fusion cross sections for Li on Co is notably
caused by breakup, but this is not the case for the Bi target.Comment: 9 pages, 9 figures, Submitted to Phys. Rev.
GaN directional couplers for integrated quantum photonics
Large cross-section GaN waveguides are proposed as a suitable architecture to
achieve integrated quantum photonic circuits. Directional couplers with this
geometry have been designed with aid of the beam propagation method and
fabricated using inductively coupled plasma etching. Scanning electron
microscopy inspection shows high quality facets for end coupling and a well
defined gap between rib pairs in the coupling region. Optical characterization
at 800 nm shows single-mode operation and coupling-length-dependent splitting
ratios. Two photon interference of degenerate photon pairs has been observed in
the directional coupler by measurement of the Hong-Ou-Mandel dip with 96%
visibility.Comment: 4 pages, 5 figure
Characterizing precursors to stellar clusters with Herschel
Context. Despite their profound effect on the universe, the formation of massive stars and stellar clusters remains elusive. Recent advances in observing facilities and computing power have brought us closer to understanding this formation process. In the past decade, compelling evidence has emerged that suggests infrared dark clouds (IRDCs) may be precursors to stellar clusters. However, the usual method for identifying IRDCs is biased by the requirement that they are seen in absorption against background mid-IR emission, whereas dust continuum observations allow cold, dense pre-stellar-clusters to be identified anywhere. Aims: We aim to understand what dust temperatures and column densities characterize and distinguish IRDCs, to explore the population of dust continuum sources that are not IRDCs, and to roughly characterize the level of star formation activity in these dust continuum sources. Methods: We use Hi-GAL 70 to 500 m bright sources at the warmest. Finally, we identify five candidate IRDC-like sources on the far-side of the Galaxy. These are cold (20 K), high column density (N(H) gt 10 cm) clouds identified with Hi-GAL which, despite bright surrounding mid-IR emission, show little to no absorption at 8 $m. These are the first inner Galaxy far-side candidate IRDCs of which the authors are aware. Herschel in an ESA space observatory with science instruments provided by European-led Principal Investigator consortia and with important participation by NASA.The FITS files discussed in the paper would be released publicly WITH the Hi-GAL data (on the Hi-GAL website) when the Hi-GAL data is released publicly.Peer reviewe
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