Raj K. Razdan
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View article: Endothelial nitric oxide synthase is regulated by ERK phosphorylation at Ser602
Endothelial nitric oxide synthase is regulated by ERK phosphorylation at Ser602 Open
eNOS (endothelial nitric oxide synthase) contains a MAPK (mitogen-activated protein kinase)-binding site associated with a major eNOS control element. Purified ERK (extracellular-signal-regulated kinase) phosphorylates eNOS with a stoichio…
View article: Synthesis of 2‐(5Z,8Z,11Z,14Z)‐Icosa‐5,8,11,14‐tetraenamidoethyl‐d<sub>4</sub> dihydrogen phosphate, tetra‐deuterated pAEA
Synthesis of 2‐(5Z,8Z,11Z,14Z)‐Icosa‐5,8,11,14‐tetraenamidoethyl‐d<sub>4</sub> dihydrogen phosphate, tetra‐deuterated pAEA Open
A labile intermediate phospho‐anandamide (2‐(5Z,8Z,11Z,14Z)‐icosa‐5,8,11,14‐tetraenamidoethyl dihydrogen phosphate, pAEA) has been identified in mouse brain and macrophages, but its precise quantitation was difficult because of its low con…
View article: Sensitivity to Δ9-tetrahydrocannabinol is selectively enhanced in beta-arrestin2−/− mice
Sensitivity to Δ9-tetrahydrocannabinol is selectively enhanced in beta-arrestin2−/− mice Open
Little is known about the roles of beta-arrestins in the regulation of brain CB1 cannabinoid receptors. This study investigated the role of beta-arrestin2 in cannabinoid behavioral effects using beta-arrestin2 -/- mice and their wild-type …
View article: Cannabinoid CB<sub>2</sub> Receptor Activation Decreases Cerebral Infarction in a Mouse Focal Ischemia/Reperfusion Model
Cannabinoid CB<sub>2</sub> Receptor Activation Decreases Cerebral Infarction in a Mouse Focal Ischemia/Reperfusion Model Open
Cannabinoid CB 2 Receptor (CB 2 ) activation has been shown to have immunomodulatory properties without psychotropic effects. The hypothesis of this study is that selective CB 2 agonist treatment can attenuate cerebral ischemia/reperfusion…
View article: The psychoactive plant cannabinoid, Δ<sup>9</sup>‐tetrahydrocannabinol, is antagonized by Δ<sup>8</sup>‐ and Δ<sup>9</sup>‐tetrahydrocannabivarin in mice<i>in vivo</i>
The psychoactive plant cannabinoid, Δ<sup>9</sup>‐tetrahydrocannabinol, is antagonized by Δ<sup>8</sup>‐ and Δ<sup>9</sup>‐tetrahydrocannabivarin in mice<i>in vivo</i> Open
Background and purpose: To follow up in vitro evidence that Δ 9 ‐tetrahydrocannabivarin extracted from cannabis (eΔ 9 ‐THCV) is a CB 1 receptor antagonist by establishing whether synthetic Δ 9 ‐tetrahydrocannabivarin (O‐4394) and Δ 8 ‐tetr…
View article: Cannabidiol displays unexpectedly high potency as an antagonist of CB<sub>1</sub>and CB<sub>2</sub>receptor agonists<i>in vitro</i>
Cannabidiol displays unexpectedly high potency as an antagonist of CB<sub>1</sub>and CB<sub>2</sub>receptor agonists<i>in vitro</i> Open
Background and purpose: A nonpsychoactive constituent of the cannabis plant, cannabidiol has been demonstrated to have low affinity for both cannabinoid CB 1 and CB 2 receptors. We have shown previously that cannabidiol can enhance electri…
View article: New potent and selective inhibitors of anandamide reuptake with antispastic activity in a mouse model of multiple sclerosis
New potent and selective inhibitors of anandamide reuptake with antispastic activity in a mouse model of multiple sclerosis Open
We previously reported that the compound O‐2093 is a selective inhibitor of the reuptake of the endocannabinoid anandamide (AEA). We have now re‐examined the activity of O‐2093 in vivo and synthesized four structural analogs (O‐2247, O‐224…
View article: CB<sub>1</sub> cannabinoid receptor‐mediated modulation of food intake in mice
CB<sub>1</sub> cannabinoid receptor‐mediated modulation of food intake in mice Open
Marijuana's appetite‐increasing effects have long been known. Recent research suggests that the CB 1 cannabinoid receptor antagonist SR141716A may suppress appetite. This study represents a further, systematic investigation of the role of …
View article: Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2‐arachidonoylglycerol
Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2‐arachidonoylglycerol Open
The pharmacology of monoacylglycerol lipase (MAGL) is not well understood. In consequence, the abilities of a series of analogues of 2‐arachidonoylglycerol (2‐AG) to inhibit cytosolic 2‐oleoylglycerol and membrane‐bound anandamide hydolysi…
View article: G Protein-coupled Endothelial Receptor for Atypical Cannabinoid Ligands Modulates a Ca2+-dependent K+ Current
G Protein-coupled Endothelial Receptor for Atypical Cannabinoid Ligands Modulates a Ca2+-dependent K+ Current Open
The cannabinoid analog “abnormal cannabidiol” (abn-cbd) causes endothelium-dependent vasodilation in rat isolated mesenteric arteries through a G protein-coupled receptor distinct from CB1 or CB2. We examined the actions of abn-cbd on the …
View article: Separation of cannabinoid receptor affinity and efficacy in delta‐8‐tetrahydrocannabinol side‐chain analogues
Separation of cannabinoid receptor affinity and efficacy in delta‐8‐tetrahydrocannabinol side‐chain analogues Open
The activities of a number of side‐chain analogues of delta‐8‐tetrahydrocannabinol (Δ 8 ‐THC) in rat cerebellar membrane preparations were tested. The affinities of each compound for the CB 1 receptor were compared by their respective abil…
View article: Novel Cannabinol Probes for CB1 and CB2 Cannabinoid Receptors
Novel Cannabinol Probes for CB1 and CB2 Cannabinoid Receptors Open
The observation that the phenolic hydroxyl of THCs was important for binding to the CB1 receptor but not as critical for binding to the CB2 receptor prompted us to extend this finding to the cannabinol (CBN) series. To study the SAR of CBN…
View article: O‐1057, a potent water‐soluble cannabinoid receptor agonist with antinociceptive properties
O‐1057, a potent water‐soluble cannabinoid receptor agonist with antinociceptive properties Open
Cannabinoids have low water solubility, necessitating the use of a solubilizing agent. In this paper we investigated whether a novel water‐soluble cannabinoid, 3‐(5′‐cyano‐1′,1′‐dimethylpentyl)‐1‐(4‐N‐morpholinobutyryloxy)‐Δ 8 ‐tetrahydroc…
View article: Comparison of novel cannabinoid partial agonists and SR141716A in the guinea‐pig small intestine
Comparison of novel cannabinoid partial agonists and SR141716A in the guinea‐pig small intestine Open
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 Δ 8 ‐tetrahydrocannabinol (Δ 8 ‐THC): O‐1184, O‐1238, O‐584 and O‐1315. These co…
View article: Cardiovascular Effects of 2-Arachidonoyl Glycerol in Anesthetized Mice
Cardiovascular Effects of 2-Arachidonoyl Glycerol in Anesthetized Mice Open
—Cannabinoids, including the endogenous ligand anandamide, elicit pronounced hypotension and bradycardia through the activation of CB1 cannabinoid receptors. A second endogenous cannabinoid, 2-arachidonoyl glycerol (2-AG), has been propose…
View article: QSAR Analysis of Δ<sup>8</sup>-THC Analogues: Relationship of Side-Chain Conformation to Cannabinoid Receptor Affinity and Pharmacological Potency
QSAR Analysis of Δ<sup>8</sup>-THC Analogues: Relationship of Side-Chain Conformation to Cannabinoid Receptor Affinity and Pharmacological Potency Open
A novel quantitative structure-activity relationship (QSAR) for the side-chain region of Delta(8)-tetrahydrocannabinol (Delta(8)-THC) analogues is reported. A series of 36 side-chain-substituted Delta(8)-THCs with a wide range of pharmacol…
View article: Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors
Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors Open
Cannabinoids, including the endogenous ligand arachidonyl ethanolamide (anandamide), elicit not only neurobehavioral but also cardiovascular effects. Two cannabinoid receptors, CB1 and CB2, have been cloned, and studies with the selective …
View article: Structural determinants of the partial agonist‐inverse agonist properties of 6′‐azidohex‐2′‐yne‐Δ<sup>8</sup>‐tetrahydrocannabinol at cannabinoid receptors
Structural determinants of the partial agonist‐inverse agonist properties of 6′‐azidohex‐2′‐yne‐Δ<sup>8</sup>‐tetrahydrocannabinol at cannabinoid receptors Open
We have extended previous investigations of four analogues of Δ 8 ‐tetrahydrocannabinol (Δ 8 ‐THC): 6′‐azidohex‐2′‐yne‐Δ 8 ‐THC (O‐1184), 6′‐azidohex‐ cis ‐2′‐ene‐Δ 8 ‐THC (O‐1238) and octyl‐2′‐yne‐Δ 8 ‐THC (O‐584) and its 1‐deoxy‐analogue…
View article: Unique Analogues of Anandamide: Arachidonyl Ethers and Carbamates and Norarachidonyl Carbamates and Ureas
Unique Analogues of Anandamide: Arachidonyl Ethers and Carbamates and Norarachidonyl Carbamates and Ureas Open
To examine the effect of changing the amide bond of anandamide (5, AN) to a less hydrolyzable moiety, analogues 1a-1l, 2a-2c, 3a-3c, and 4a-4h were synthesized from commercially available arachidonyl alcohol or arachidonic acid and tested …
View article: An investigation into the structural determinants of cannabinoid receptor ligand efficacy
An investigation into the structural determinants of cannabinoid receptor ligand efficacy Open
A number of side‐chain analogues of Δ 8 ‐THC were tested in GTPγS binding assay in rat cerebellar membranes. O‐1125, a saturated side‐chain compound stimulated GTPγS binding with an E max of 165.0%, and an EC 50 of 17.4 n M . O‐1236, O‐123…
View article: Comparison of cannabinoid binding sites in guinea‐pig forebrain and small intestine
Comparison of cannabinoid binding sites in guinea‐pig forebrain and small intestine Open
We have investigated the nature of cannabinoid receptors in guinea‐pig small intestine by establishing whether this tissue contains cannabinoid receptors with similar binding properties to those of brain CB 1 receptors. The cannabinoids us…