The preparation of 5′‐iodo‐<sup>125</sup>I‐Δ<sup>8</sup>‐THC; a radioligand for the radioimmunoassay of cannabinoids

Pitt, Colin G.; Seltzman, Herbert H.; Setzer, Susan R.; Williams, David L.

doi:10.1002/jlcr.2580170510

Cited by 10 publications

(3 citation statements)

References 7 publications

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“…All blood was immediately centrifuged, and the plasma supernatant was frozen (-20°C) until the assay. Samples were assayed by established radioimmunoassay techniques [40][41][42] at the Research Triangle Institute (Research Triangle Park, NC). Sensitivity of the assay was 2 ng/mL, and the coefficient of variation for control samples at both 8 and 30 ng/mL was less than 10% for all assay runs.…”

Section: Methodsmentioning

confidence: 99%

Effect of Acute Marijuana on Cardiovascular Function and Central Nervous System Pharmacokinetics of [15O]Water: Effect in Occasional and Chronic Users

Ponto

O'Leary

Koeppel

et al. 2004

The Journal of Clinical Pharma

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The objective of this study was to evaluate the effect of the acute administration of marijuana (MJ) on cardiovascular (CV) function and CNS pharmacokinetics (PK) of [(15)O]water in occasional (O) versus chronic (C) MJ users. Each subject received four injections of [(15)O]water (one prior and three postsmoking) on two occasions in which they received active or placebo MJ. For each injection, measures of CV function and CNS PK [(15)O]water were made. Postsmoking, MJ influenced all measured CV and [(15)O]water PK parameters. C users reported significantly lower "highness" and smaller heart rate (HR) changes, which resulted in reduced rate pressure product (RPP) changes compared to O users, even though Delta(9)-tetrahydrocannabinol levels were higher, whereas changes in blood pressure (BP), arrival time, and [(15)O]water concentration were not significantly different between the groups. Significant CV changes resulted in changes in the whole-body distribution of cardiac output rather than changes in cerebral blood flow. Chronic MJ use produces tolerance to the HR increases induced by acute MJ smoking compared to changes observed in occasional users, without changing the effects on BP and [(15)O]water PK.

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Section: Methodsmentioning

confidence: 99%

Effect of Acute Marijuana on Cardiovascular Function and Central Nervous System Pharmacokinetics of [15O]Water: Effect in Occasional and Chronic Users

Ponto

O'Leary

Koeppel

et al. 2004

The Journal of Clinical Pharma

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“…As mentioned, the tosylate group was successfully used for iodination of heptadecanoic acid [49,50], but failed in other cases [54]. Organic leaving groups have been successfully used to prepare 12S Ι-Δ 8 -tetrahydrocannabinol via the tosylate [55], and 77 Br-and I25 Inorhexestrol via the triflate [56], with specific activities of > 1600 Ci/mmole and 130 Ci/mmole, respectively. A triflate precursor was also applied for the n.c.a.…”

Section: Exchange Of Halogen and Organic Substituentsmentioning

confidence: 96%

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

1983

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Radiolabeling methods with the heavy halogens bromine, iodine and astatine are reviewed. The methods are evaluated on the basis of their underlying chemical principles and their usefulness for the no-carrier-added labeling of biologically-useful compounds. Special emphasis is placed on the stability, specific activity, and quality control of radiohalogenation products using the shortlived, neutron-deficient nuclides 7s ' 7 'Br, '"I, and 2 "At in view of their importance as radiopharmaceuticals.

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“…In 1964, THC was identified as a CB 1 receptor ligand, and soon after it was 14 C-labeled to provide the first CB receptor radioligand [ 14 C]THC (Miras, 1965). Since then a number of THC-based CB receptor radioligands have been developed (Agurell et al, 1969;Pitt et al, 1980;Nye et al, 1985); however, nowadays these are not commonly used due to high nonspecific membrane binding.…”

Section: B Applications Of Radioligandsmentioning

confidence: 99%

Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors

Cooper

Singh

Hook

et al. 2017

Pharmacological Reviews

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Cannabinoid, free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid, leukotriene, bile acid, and platelet-activating factor receptor families are class A G protein-coupled receptors with endogenous lipid ligands. Pharmacological tools are crucial for studying these receptors and addressing the many unanswered questions surrounding expression of these receptors in normal and diseased tissues. An inherent challenge for developing tools for these lipid receptors is balancing the often lipophilic requirements of the receptor-binding pharmacophore with favorable physicochemical properties to optimize highly specific binding. In this study, we review the radioligands, fluorescent ligands, covalent ligands, and antibodies that have been used to study these lipid-binding receptors. For each tool type, the characteristics and design rationale along with in vitro and in vivo applications are detailed.

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The preparation of 5′‐iodo‐¹²⁵I‐Δ⁸‐THC; a radioligand for the radioimmunoassay of cannabinoids

Cited by 10 publications

References 7 publications

Effect of Acute Marijuana on Cardiovascular Function and Central Nervous System Pharmacokinetics of [15O]Water: Effect in Occasional and Chronic Users

Effect of Acute Marijuana on Cardiovascular Function and Central Nervous System Pharmacokinetics of [15O]Water: Effect in Occasional and Chronic Users

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors

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The preparation of 5′‐iodo‐125I‐Δ8‐THC; a radioligand for the radioimmunoassay of cannabinoids

Cited by 10 publications

References 7 publications

Effect of Acute Marijuana on Cardiovascular Function and Central Nervous System Pharmacokinetics of [15O]Water: Effect in Occasional and Chronic Users

Effect of Acute Marijuana on Cardiovascular Function and Central Nervous System Pharmacokinetics of [15O]Water: Effect in Occasional and Chronic Users

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors

Contact Info

Product

Resources

About

The preparation of 5′‐iodo‐¹²⁵I‐Δ⁸‐THC; a radioligand for the radioimmunoassay of cannabinoids