Radioligand Assay

Publication Title: 
Biological Psychiatry

BACKGROUND: Prenatal cannabis exposure has been linked to addiction vulnerability, but the neurobiology underlying this risk is unknown. METHODS: Striatal dopamine and opioid-related genes were studied in human fetal subjects exposed to cannabis (as well as cigarettes and alcohol). Cannabis-related gene disturbances observed in the human fetus were subsequently characterized with an animal model of prenatal ?-9-tetrahydrocannabinol (THC) (.15 mg/kg) exposure.

Author(s): 
DiNieri, Jennifer A.
Wang, Xinyu
Szutorisz, Henrietta
Spano, Sabrina M.
Kaur, Jasbir
Casaccia, Patrizia
Dow-Edwards, Diana
Hurd, Yasmin L.
Publication Title: 
Methods and Findings in Experimental and Clinical Pharmacology

The general pharmacological profile and effects of E-4716 on the CNS have been investigated in comparison with other histamine receptor blockers. In in vitro studies with isolated organs and in binding studies on numerous receptors, E-4716 had no activity even at high concentrations, except for the selective blockade of H1 receptors. No activity was observed in pharmacological trials in vivo, such as the Irwin test or analgesia induced by phenylbenzoquinone or electroshock, suggesting a depressant activity on the CNS.

Author(s): 
Fisas, M. A.
Gutiérrez, B.
Fort, M.
Dordal, A.
García, C.
Farré, A. J.
Publication Title: 
Anesthesiology

BACKGROUND: Propofol can be associated with delayed awakening after prolonged infusion. The aim of this study was to characterize the preclinical pharmacology of AZD-3043, a positive allosteric modulator of the ?-aminobutyric acid type A (GABA(A)) receptor containing a metabolically labile ester moiety. The authors postulated that its metabolic pathway would result in a short-acting clinical profile. METHODS: The effects of AZD-3043, propofol, and propanidid were studied on GABA(A) receptor-mediated chloride currents in embryonic rat cortical neurons.

Author(s): 
Egan, Talmage D.
Obara, Shinju
Jenkins, Thomas E.
Jaw-Tsai, Sarah S.
Amagasu, Shanti
Cook, Daniel R.
Steffensen, Scott C.
Beattie, David T.
Publication Title: 
Biochemical and Biophysical Research Communications

Limonene is a major aromatic compound in essential oils extracted from citrus rind. The application of limonene, especially in aromatherapy, has expanded significantly, but its potential effects on cellular metabolism have been elusive. We found that limonene directly binds to the adenosine A(2A) receptor, which may induce sedative effects. Results from an in vitro radioligand binding assay showed that limonene exhibits selective affinity to A(2A) receptors.

Author(s): 
Park, Hyo Min
Lee, Ji Hae
Yaoyao, Jia
Jun, Hee Jin
Lee, Sung Joon
Publication Title: 
Medicinal Research Reviews

Traditional medicinal plants in various countries, particularly in India have been used for centuries for various ailments; however, there has been little scientific effort to validate these anecdotal uses mentioned in the literature.

Author(s): 
Misra, R.
Publication Title: 
Anticancer Research

The peripheral-type benzodiazepine receptor (PBR) is an 18-kDa high affinity drug- and cholesterol-binding protein that is involved in various cell functions, including cell proliferation and apoptosis. PBR was shown to be overexpressed in certain types of malignant human tumors and cancer cell lines, correlating with enhanced tumorigenicity and cell proliferation rates. The present study was conducted in order to further define the role of PBR in cancer and to extend our recent findings regarding the possible anticancer effects of the standardized Ginkgo biloba extract EGb 761.

Author(s): 
Pretner, Ewald
Amri, Hakima
Li, Wenping
Brown, Rachel
Lin, Chin-Shoou
Makariou, Erini
Defeudis, Francis V.
Drieu, Katy
Papadopoulos, Vassilios
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

(E)-Methyl 2-((2S,3S,7aS,12bS)-3-ethyl-7a-hydroxy-8-methoxy-1,2,3,4,6,7,7a,12b-octahydroindolo[2,3-a]quinolizin-2-yl)-3-methoxyacrylate (7-hydroxymitragynine), a main active constituent of the traditional herbal medicine Mitragyna speciosa, is an indole alkaloid that is structurally different from morphine. 7-Hydroxymitragynine induces a potent antinociceptive effect on mouse acute pain through μ-opioid receptors. In this study, we developed dual-acting μ- and δ-opioid agonists MGM-15 and MGM-16 from 7-hydroxymitragynine for the treatment of acute and chronic pain.

Author(s): 
Matsumoto, Kenjiro
Narita, Minoru
Muramatsu, Naotaka
Nakayama, Terumi
Misawa, Kaori
Kitajima, Mariko
Tashima, Kimihito
Devi, Lakshmi A.
Suzuki, Tsutomu
Takayama, Hiromitsu
Horie, Syunji
Publication Title: 
Chinese Medical Journal
Author(s): 
Zhang, A. Z.
Pan, X. P.
Xu, S. F.
Cheng, J. S.
Mo, W. Y.
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