Scientific Articles Repository
This section is dedicated to all the scientific articles that we consider related to our domains of expertise and those of our affiliates.
Chemistry:
- Potential drug abuse therapeutics derived from the hallucinogenic natural product salvinorin A
By Katherine M. Prevatt-Smith, Kimberly M. Lovell, Denise S. Simpson, Victor W. Day, Justin T. Douglas, Peter Bosch, Christina M. Dersch, Richard B. Rothman, Bronwyn Kivell and Thomas E. Prisinzano
Previous structure–activity relationship studies of salvinorin A have shown that modification of the acetate functionality off the C-2 position to a methoxy methyl or methoxy ethyl ether moiety leads to increased potency at KOP receptors. However, the reason for this increase remains unclear. Here we report our efforts towards the synthesis and evaluation of C-2 constrained analogs of salvinorin A. These analogs were evaluated at opioid receptors in radioligand binding experiments as well as in the GTP-g-S functional assay. One compound, 5, was found to have affinity and potency at k opioid (KOP) receptors comparable to salvinorin A. In further studies, 5 was found to attenuate cocaine-induced drug seeking behavior in rats comparably to salvinorin A. This finding represents the first example of a salvinorin A analog that has demonstrated anti-addictive capabilities.
DOI: 10.1039/c1md00192b
https://sci-hub.se/10.1039/c1md00192b - Synthesis and in vitro pharmacological studies of new C(2)modified salvinorin A analogues
By David Y.W. Lee, Vishnu V.R. Karnati, Minsheng He, Lee-Yuan Liu-Chen, Leelakrishna Kondaveti, Zhongze Ma, Yulin Wang, Yong Chen, Cecile Beguin, William A. Carlezon, Jr. and Bruce Cohen
Salvinorin A is the most potent naturally occurring opioid agonist yet discovered with high selectivity and affinity for j-opioid receptor. To explore its structure and activity relationships, a series of salvinorin A derivatives modified at the C(2) position were prepared and studied. These salvinorin A derivatives were screened for binding and functional activities at the human j-opioid receptor. Compound 4, containing a methoxymethyl group at the 2-position, was a full j-agonist with an EC 50 value at 0.6 nM, which is about 7 times more potent than salvinorin A.
DOI: 10.1016/j.bmcl.2005.05.048
https://sci-hub.se/https://doi.org/10.1016/j.bmcl.2005.05.048 - Detection and characterization of emerging psychoactive substances by ion mobility spectrometry
By Sergio Armenta, Salvador Garrigues, Miguel de la Guardia, Judit Brassier, Manel Alcalà, Marcelo Blanco, Clara Perez-Alfonso and Nieves Galipienso
Rapid detection and identification of novel psychoactive substances (NPS) continues to present significant analytical challenges to forensic and analytical chemists. Ion mobility spectrometry (IMS) has been traditionally considered as the analytical technique of choice to detect illicit drugs in security points in airports, borderlines and customs. Databases of the reduced mobility (K 0 ) values of illicit drugs are available in the scientific literature and they should be completed with data of emerging designer drugs. In this paper, we have evaluated the effect of different measurement conditions and determined the K 0 values of an important number of NPS including different families; such as phenethylamines, cathinones, synthetic cannabinoids and tryptamines among others to be incorporated to the existing data to provide a rapid detection and identification of this emerging threat.
DOI: 10.1002/dta.1678
https://sci-hub.se/10.1002/dta.1678Pharmacology:
- N/A
Biology:
- Modified Oligonucleotides: Synthesis and Strategy for Users - Sandeep Verma and Fritz Eckstein Max-Planck-Institut fur Experimentelle Medizin, Hermann-Rein Strasse 3, D-37075 G¨ottingen, Germany
Synthetic oligonucleotide analogs have greatly aided our understanding of sev-
eral biochemical processes. Efficient solid-phase and enzyme-assisted synthetic
methods and the availability of modified base analogs have added to the utility
of such oligonucleotides. In this review, we discuss the applications of synthetic
oligonucleotides that contain backbone, base, and sugar modifications to inves-
tigate the mechanism and stereochemical aspects of biochemical reactions. We
also discuss interference mapping of nucleic acid–protein interactions; spectro-
scopic analysis of biochemical reactions and nucleic acid structures; and nucleic
acid cross-linking studies.
The automation of oligonucleotide synthesis, the development of versatile
phosphoramidite reagents, and efficient scale-up have expanded the application
of modified oligonucleotides to diverse areas of fundamental and applied bi-
ological research. Numerous reports have covered oligonucleotides for which
modifications have been made of the phosphodiester backbone, of the purine and
pyrimidine heterocyclic bases, and of the sugar moiety; these modifications serve
as structural and mechanistic probes. In this chapter, we review the range, scope,
and practical utility of such chemically modified oligonucleotides. Because of
space limitations, we discuss only those oligonucleotides that contain phosphate
and phosphate analogs as internucleotidic linkages.
DOI: 10.1146/annurev.biochem.67.1.99
https://sci-hub.se/10.1146/annurev.biochem.67.1.99Biometrics:
- Fingerprint Alteration - Jianjiang Feng, Anil K. Jain, and Arun Ross
The widespread deployment of Automated Fingerprint Identification Systems (AFIS) in law enforcement and border control applications has heightened the need for ensuring that
the security afforded by these systems is not compromised. While
several issues related to fingerprint system security have been
investigated in the past, including the use of fake fingerprints for
masquerading identity, the problem of fingerprint alteration or
obfuscation has received no attention in the biometric literature.
Fingerprint obfuscation refers to the deliberate alteration of the
fingerprint pattern by an individual for the purpose of masking
his or her identity. Several cases of fingerprint obfuscation have
been described in the media. Existing image quality assessment
software cannot detect such altered fingerprints since the implicit
image quality during alteration may not change significantly.
The goal of this paper is to understand the problem of altered
fingerprints and to design solutions that can be used to detect these images.