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J W Huffman et al.
Life sciences, 56(23-24), 2021-2024 (1995-01-01)
The synthesis of (2'RS)-2'-methyl-, (3'RS)-, (3'S)-3'-methyl-, and 4'-methyl-delta 8-THC has been carried out, and the pharmacology of all four compounds has been investigated. All four compounds showed typical cannabinoid activity both in vitro and in vivo. The 2'-methyl compound is
Abir T El-Alfy et al.
Pharmacology, biochemistry, and behavior, 95(4), 434-442 (2010-03-25)
The antidepressant action of cannabis as well as the interaction between antidepressants and the endocannabinoid system has been reported. This study was conducted to assess the antidepressant-like activity of Delta(9)-THC and other cannabinoids. Cannabinoids were initially evaluated in the mouse
T Mavromoustakos et al.
Biochimica et biophysica acta, 1420(1-2), 252-265 (1999-08-14)
The thermotropic and dynamic properties of the biologically active Delta(8)-tetrahydrocannabinol (Delta(8)-THC) and its inactive congener O-methyl-Delta(8)-tetrahydrocannabinol (Me-Delta(8)-THC) in DPPC/cholesterol (CHOL) bilayers have been studied using a combination of DSC and solid-state NMR spectroscopy. The obtained results showed differential effects of
Donna A Whyte et al.
Pharmacology, 85(6), 328-335 (2010-06-03)
The primary cannabinoids, Delta(9)-tetrahydrocannabinol (Delta(9)-THC) and Delta(8)-tetrahydrocannabinol (Delta(8)-THC) are known to disturb the mitochondrial function and possess antitumor activities. These observations prompted us to investigate their effects on the mitochondrial O(2) consumption in human oral cancer cells (Tu183). This epithelial
P Consroe et al.
Pharmacology, biochemistry, and behavior, 40(3), 517-522 (1991-11-01)
Plasma levels of cannabidiol (CBD) were ascertained weekly in 14 Huntington's disease patients undergoing a double-blind, placebo-controlled, crossover trial of oral CBD (10 mg/kg/day = about 700 mg/day) for 6 weeks. The assay procedure involved trimethylsilyl (TMS) derivatization of CBD
P R Stout et al.
Journal of analytical toxicology, 24(7), 567-571 (2000-10-24)
The loss of delta9-tetrahydrocannabinol (THCCOOH) from urine specimens stored in polypropylene and polyethylene containers at 4 degrees C and 25 degrees C was examined. All specimens were analyzed by GC-MS after sampling at various times over a one-week period. Data
Ketan Hippalgaonkar et al.
AAPS PharmSciTech, 12(2), 723-731 (2011-06-04)
The purpose of this study was to investigate the effect of cyclodextrins (CDs) on aqueous solubility, stability, and in vitro corneal permeability of delta-8-tetrahydrocannabinol (Δ(8)-THC). Phase solubility of Δ(8)-THC was studied in the presence of 2-hydroxypropyl-β-cyclodextrin (HPβCD), randomly methylated-β-cyclodextrin (RMβCD)
S H Burstein et al.
Life sciences, 56(23-24), 1991-1998 (1995-01-01)
Binding and photoactivation of a cannabinoid-derived ligand to intact mouse peritoneal cells has resulted in the labelling of a G-protein gamma-subunit. The assignment of structure is based on the product's physical characteristics and its ability to react with a polyclonal
A A Coutts et al.
British journal of pharmacology, 129(4), 645-652 (2000-02-22)
The controversial nature of the CB(1) receptor antagonist, SR141716A, in the guinea-pig small intestine was investigated by comparing it with four analogues of Delta(8)-tetrahydrocannabinol (Delta(8)-THC): O-1184, O-1238, O-584 and O-1315. These compounds (10 - 1000 nM) inhibited the electrically-evoked contractions
S Muchtar et al.
Ophthalmic research, 24(3), 142-149 (1992-01-01)
delta 8-Tetrahydrocannabinol (delta 8-THC), a known antiglaucoma lipophilic drug, was incorporated in a submicron emulsion for ocular administration. The mean droplet size of the emulsion was 130 +/- 41 nm, and no droplet was larger than 400 nm. No change
B R Martin et al.
Pharmacology, biochemistry, and behavior, 46(2), 295-301 (1993-10-01)
One aspect of cannabinoid structure-activity relationships (SARs) that has not been thoroughly investigated is the aromatic (A) ring. Although halogenation of the side chain enhances potency, our recent observation that iodination of the A ring also enhanced activity was surprising.
D P Yang et al.
Biochimica et biophysica acta, 1103(1), 25-36 (1992-01-10)
The effects of (-)-delta 8-tetrahydrocannabinol (delta 8-THC) and its biologically inactive O-methyl ether analog on model phospholipid membranes were studied using a combination of differential scanning calorimetry (DSC), small angle X-ray diffraction and solid state 2H-NMR. The focus of this
Spyros P Nikas et al.
The AAPS journal, 6(4), e30-e30 (2005-03-12)
The presence of halogens within the classical cannabinoid structure leads to large variations in the compounds' potencies and affinities for the CB1 receptors. To explore the structure activity relationships within this class of analogs we have used a series of
A D Khanolkar et al.
Bioorganic & medicinal chemistry letters, 9(15), 2119-2124 (1999-08-28)
Novel analogs of (-)-delta8-tetrahydrocannabinol (delta8-THC) in which the conformation of the side chain was restricted by incorporating the first one or two carbons into a six membered ring fused with the aromatic phenolic A ring were synthesized. The affinities of
David Andersen et al.
Journal of analytical toxicology, 36(4), 280-287 (2012-04-05)
A fully automated setup was developed for preparing whole blood samples using a Tecan Evo workstation. By integrating several add-ons to the robotic platform, the flexible setup was able to prepare samples from sample tubes to a 96-well sample plate
A Charalambous et al.
Pharmacology, biochemistry, and behavior, 40(3), 509-512 (1991-11-01)
-(-)-5'-Bromo-delta 8-THC, (-)-5'-trifluoromethyl-delta 8-THC, (-)-5'-iodo-delta 8-THC, (-)-5'-fluoro-delta 8-THC, (-)-11-fluoro-delta 8-THC and (-)-2-iodo-delta 8-THC were synthesized and evaluated in male ICR mice for their effects on sedation, temperature, catalepsy and antinociception following intravenous injection. The analogs were also tested for relative
A Abrahamov et al.
Life sciences, 56(23-24), 2097-2102 (1995-01-01)
Delta-8-tetrahydrocannabinol (delta-8-THC), a cannabinoid with lower psychotropic potency than the main Cannabis constituent, delta-9-tetrahydrocannabinol (delta-9-THC), was administered (18 mg/m2 in edible oil, p.o.) to eight children, aged 3-13 years with various hematologic cancers, treated with different antineoplastic drugs for up
Taku Yamaguchi et al.
Journal of neurochemistry, 88(1), 148-154 (2003-12-17)
We have previously shown that behavioral changes induced by cannabinoid were due to an elevation of prostaglandin E2 (PGE2) via the arachidonic acid cascade in the brain. In the present study, we investigated the participation of the prostanoid EP3 receptor
Christian D Schubart et al.
Schizophrenia research, 130(1-3), 216-221 (2011-05-20)
Cannabis is associated with psychotic outcomes in numerous studies, an effect that is commonly attributed to Δ (9)-tetrahydrocannabinol (Δ 9-THC). An increasing number of authors identify cannabidiol, another component of the cannabis plant, as an antipsychotic agent. The objective of
Audra L Stinchcomb et al.
The Journal of pharmacy and pharmacology, 56(3), 291-297 (2004-03-18)
The purpose of this study was to quantify the in-vitro human skin transdermal flux of Delta8-tetrahydrocannabinol (Delta8-THC), cannabidiol (CBD) and cannabinol (CBN). These cannabinoids are of interest because they are likely candidates for transdermal combination therapy. Differential thermal analysis and
Satyanarayana Valiveti et al.
Journal of pharmaceutical sciences, 93(5), 1154-1164 (2004-04-07)
The present study was carried out in order to develop a transdermal therapeutic system (TTS) for Delta(8)-THC. The in vitro permeability studies of Delta(8)-THC in human skin and hairless guinea pig skin with and without a rate-controlling membrane were conducted
Nissar A Darmani et al.
European journal of pharmacology, 563(1-3), 187-196 (2007-03-17)
Xenobiotic cannabinoid CB1/CB2-receptor agonists appear to possess broad-spectrum antiemetic activity since they prevent vomiting produced by a variety of emetic stimuli including the chemotherapeutic agent cisplatin, serotonin 5-HT3-receptor agonists, dopamine D2/D3-receptor agonists and morphine, via the stimulation of CB1-receptors. The
T Mavromoustakos et al.
Pharmacology, biochemistry, and behavior, 40(3), 547-552 (1991-11-01)
In a previous publication, we have described in detail how we used small angle x-ray diffraction to determine the topography of (-)-delta 8-tetrahydrocannabinol (delta 8-THC) in dimyristoylphosphatidylcholine (DMPC) bilayers, and to deduce the conformation of the THC side chain by
R A Hirst et al.
Neuroscience letters, 220(2), 101-104 (1996-12-13)
We describe the use of SR141716A, a central cannabinoid antagonist, in radioligand binding and adenylyl cyclase (AC) inhibition studies in rat cerebella membranes. The binding of [3H]SR141716A was dose-dependent and saturable, with Kd and Bmax of 0.61 +/- 0.12 nM
I Wirguin et al.
Immunopharmacology, 28(3), 209-214 (1994-11-01)
The effect of delta 8-THC on experimental autoimmune encephalomyelitis (EAE) was examined. delta 8-THC is an analogue of delta 9-THC, the psychoactive component of marijuana. It is more stable and less psychotropic than delta 9-THC and like the latter it
Dong Joon Kim et al.
Cancer research, 72(12), 3060-3068 (2012-04-24)
The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell-originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation. Despite the identification of TOPK as a promising novel therapeutic target, no inhibitor of TOPK has
C Cajado et al.
Cytokine, 56(2), 312-317 (2011-08-02)
Sickle cell anemia (SCA) is a disorder characterized by a heterogeneous clinical outcome. In the present study, we investigated the associations between Tumor Necrosis Factor-alpha (TNF-alpha) -308G>A and Interleukin 8 (IL-8) -251A>T gene polymorphisms, medical history and classical biomarkers in
Khomsan Supong et al.
International journal of systematic and evolutionary microbiology, 63(Pt 11), 3970-3974 (2013-05-28)
An actinomycete strain, SP03-05(T), was isolated from a marine sponge sample (Xestospongia sp.) collected from Phuket Province of Thailand. The strain was aerobic, Gram-stain-positive and produced single spores at the tips of the substrate mycelium. Strain SP03-05(T) contained meso-diaminopimelic acid
Zohreh Rahimi et al.
Angiology, 63(2), 131-137 (2011-05-24)
There are conflicting reports about the association of endothelial nitric oxide synthase (eNOS) gene polymorphism and the risk of coronary artery disease (CAD). To determine the frequency of eNOS G894T variant and to find the possible association between this polymorphism
Laura R Iwasaki et al.
American journal of orthodontics and dentofacial orthopedics : official publication of the American Association of Orthodontists, its constituent societies, and the American Board of Orthodontics, 130(6), 698-698 (2006-12-16)
The variables affecting speed of tooth movement are unquantified. In particular, the effects of stress and human biological variations are unknown. Therefore, our objectives in this study were to determine relationships between (1) stress and velocity of tooth translation (v(t))
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