The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents

Author(s):  
Muhammed Alzweiri ◽  
Amsha Alsegiani ◽  
Endri Karaj ◽  
Daniyah Almarghalani ◽  
Yahia Tabaza ◽  
...  
2021 ◽  
pp. 1-6
Author(s):  
Matthijs Blankers ◽  
Daan van der Gouwe ◽  
Lavinia Stegemann ◽  
Laura Smit-Rigter

<b><i>Background:</i></b> In this article, we present an evaluation of online psychoactive substance trade via Telegram, a free encrypted social media messenger service. The evaluation took place during the COVID-19 pandemic, which allowed us to monitor the effects of the spring 2020 lockdown in the Netherlands on substance trade via Telegram. <b><i>Objective:</i></b> The objective of this study was to evaluate whether changes in psychoactive substance trade on Telegram markets in the Netherlands can be observed during the COVID-19 pandemic. <b><i>Results:</i></b> Between December 2, 2019, and June 29, 2020, a total of 70,226 posts appeared in two analyzed Telegram groups. A total of 5,643 posts were psychoactive substance related. Based on the analyzed posts, Telegram is mostly a ‘“sellers” market as only a minority of the posts (6.3%) could be identified as a request for a substance. The proportion of posts related to specific substances varied between the periods before, during, and after the lockdown. The proportion of posts on the stimulants ecstasy, cocaine, and amphetamine was lower during the lockdown than before and after. For psychedelics – ketamine, lysergic acid diethylamide (LSD), and 2,5-dimethoxy-4-bromophenethylamine (2C-B) – and other substances, there was a relative increase in the number of posts during the lockdown, which was maintained after the lockdown. <b><i>Conclusions:</i></b> Telegram analysis shows that in the Netherlands, online psychoactive substance trade may have been affected during the COVID-19 pandemic. The direction of this effect was different for different classes of substances.


1960 ◽  
Vol 198 (3) ◽  
pp. 543-546 ◽  
Author(s):  
S. A. Kabins ◽  
J. Fridman ◽  
J. Neustadt ◽  
G. Espinosa ◽  
L. N. Katz

A localized pulmonary infarction was produced by injecting a starch suspension into the pulmonary artery wedge position of one lung lobe in pentobarbitalized dogs, and the effect of three so-called antiserotonins on the ensuing pulmonary edema was determined. Edema was inhibited in the nonembolized lung lobes in 88% of the B.A.S. (1-benzyl-2-methyl-5-methoxytryptamine HCl), 45% of the DHE (dihydroergotamine), and 12% of the BOL (2-brom- d-lysergic acid diethylamide) dogs. Reasons are given for assuming that the actions of B.A.S. and DHE are due to their antiadrenergic rather than to any antiserotonin properties which they may have. Serotonin, therefore, at most has a slight role in the pulmonary edema formation caused by starch emboli. It is postulated that the emboli by producing an infarct and setting up a reflex mediated through the sympathetic nervous system, cause the release in turn of catecholamines and of histamine, the latter being immediately responsible for the capillary permeability change leading to pulmonary edema.


Science ◽  
1957 ◽  
Vol 126 (3281) ◽  
pp. 1020-1020 ◽  
Author(s):  
H. A. ABRAMSON ◽  
B. SKLAROFSKY ◽  
M. O. BARON ◽  
N. FREMONT-SMITH

1997 ◽  
Vol 4 (5) ◽  
pp. 211 ◽  
Author(s):  
Kari Blaho ◽  
Kevin Merigian ◽  
Stephen Winbery ◽  
Stephen A. Geraci ◽  
Chantay Smartt

Heterocycles ◽  
2007 ◽  
Vol 71 (5) ◽  
pp. 1075 ◽  
Author(s):  
István Moldvai ◽  
Luca Russo ◽  
Kari Rissanen ◽  
Julianna Kardos ◽  
Eszter Gács-Baitz ◽  
...  
Keyword(s):  

2014 ◽  
Vol 80 (20) ◽  
pp. 6465-6472 ◽  
Author(s):  
Sarah L. Robinson ◽  
Daniel G. Panaccione

ABSTRACTDifferent lineages of fungi produce distinct classes of ergot alkaloids. Lysergic acid-derived ergot alkaloids produced by fungi in the Clavicipitaceae are particularly important in agriculture and medicine. The pathway to lysergic acid is partly elucidated, but the gene encoding the enzyme that oxidizes the intermediate agroclavine is unknown. We investigated two candidate agroclavine oxidase genes from the fungusEpichloë festucaevar.lolii×Epichloë typhinaisolate Lp1 (henceforth referred to asEpichloësp. Lp1), which produces lysergic acid-derived ergot alkaloids. Candidate geneseasHandcloAwere expressed in a mutant strain of the moldAspergillus fumigatus, which typically produces a subclass of ergot alkaloids not derived from agroclavine or lysergic acid. Candidate genes were coexpressed with theEpichloësp. Lp1 allele ofeasA, which encodes an enzyme that catalyzed the synthesis of agroclavine from anA. fumigatusintermediate; the agroclavine then served as the substrate for the candidate agroclavine oxidases. Strains expressingeasAandcloAfromEpichloësp. Lp1 produced lysergic acid from agroclavine, a process requiring a cumulative six-electron oxidation and a double-bond isomerization. Strains that accumulated excess agroclavine (as a result ofEpichloësp. Lp1easAexpression in the absence ofcloA) metabolized it into two novel ergot alkaloids for which provisional structures were proposed on the basis of mass spectra and precursor feeding studies. Our data indicate that CloA catalyzes multiple reactions to produce lysergic acid from agroclavine and that combining genes from different ergot alkaloid pathways provides an effective strategy to engineer important pathway molecules and novel ergot alkaloids.


ChemInform ◽  
2010 ◽  
Vol 25 (9) ◽  
pp. no-no
Author(s):  
Y. OZLU ◽  
D. E. CLADINGBOEL ◽  
P. J. PARSONS
Keyword(s):  

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