scholarly journals Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain

2021 ◽  
Vol 22 (15) ◽  
pp. 8051
Author(s):  
Rodrigo Teodoro ◽  
Daniel Gündel ◽  
Winnie Deuther-Conrad ◽  
Lea Ueberham ◽  
Magali Toussaint ◽  
...  
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Biological Evaluation ◽  
Emission Tomography ◽  
Tailored Therapy ◽  
Positron Emission ◽  
Cannabinoid Receptor Type 2 ◽  
Attractive Therapeutic Target ◽  
The Brain

Cannabinoid receptors type 2 (CB2R) represent an attractive therapeutic target for neurodegenerative diseases and cancer. Aiming at the development of a positron emission tomography (PET) radiotracer to monitor receptor density and/or occupancy during a CB2R-tailored therapy, we herein describe the radiosynthesis of cis-[18F]1-(4-fluorobutyl-N-((1s,4s)-4-methylcyclohexyl)-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide ([18F]LU14) starting from the corresponding mesylate precursor. The first biological evaluation revealed that [18F]LU14 is a highly affine CB2R radioligand with >80% intact tracer in the brain at 30 min p.i. Its further evaluation by PET in a well-established rat model of CB2R overexpression demonstrated its ability to selectively image the CB2R in the brain and its potential as a tracer to further investigate disease-related changes in CB2R expression.

scholarly journals Premature delivery and cannabinoid receptor expression in the placenta after delivery: an observational study.

2020 ◽  
Author(s):  
Stepan Feduniw ◽  
Izabela Woś ◽  
Katarzyna Pogoda ◽  
Piotr Laudanski ◽  
Jacek Tabarkiewicz ◽  
...  
Keyword(s):  
Preterm Delivery ◽  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Receptor Expression ◽  
Receptor Type ◽  
Premature Delivery ◽  
Study Group ◽  
Cannabinoid Receptor Type 2 ◽  
History Of

Objective: To investigate the relationship between cannabinoid receptor expression within the placenta after delivery and the problem of preterm delivery. Design, setting, and participants: The retrospective, observational study was conducted on a multicenter material of 150 women. The study group included 115 women after premature delivery. The control group consisted of 35 women after term delivery. Methods. To determine the expression of cannabinoid receptors after the end of the third stage of labour, several sections were taken from the placenta. RNA isolation, reverse transcription, and Real-Time PCR were performed to assess the expression of the cannabinoid receptors in the placenta. Results: Cannabinoid receptor type 2 expression was lower in the placentas of women after preterm delivery. Urinary tract infections and bleeding at any stage of pregnancy occurred statistically more frequently in the study group and correlated with cannabinoid receptor type 2 expression. In the study group, the history of preterm labor, history of intrauterine fetal deaths, pregnancies terminated by a Caesarean section, and uterine tenderness correlated with lower expression of cannabinoid receptor type 2 and 1a. Conclusions: Cannabinoid receptors mRNA were present in human placental tissue during pregnancy. Decreased cannabinoid receptor type 2 expression in preterm delivered placentas should be further investigated, as perinatal endocannabinoid receptor expression could serve as a predicting tool of preterm birth. For example, liquid-based cytology could be used as a noninvasive perinatal method of measuring the expression level of cannabinoid receptors in decidual cells during pregnancy. KEYWORDS: Cannabinoid receptor; CB2; endocannabinoid system; preterm delivery; PTB

scholarly journals Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands

Molecules ◽  
2017 ◽  
Vol 22 (1) ◽  
pp. 77 ◽  
Author(s):  
Rareş-Petru Moldovan ◽  
Winnie Deuther-Conrad ◽  
Andrew Horti ◽  
Peter Brust
Keyword(s):  
Cannabinoid Receptor ◽  
Biological Evaluation ◽  
Receptor Type ◽  
Cannabinoid Receptor Type 2

Amyloid and Tau Positron Emission Tomography in Suggested Diabetesrelated Dementia

2018 ◽  
Vol 15 (11) ◽  
pp. 1062-1069 ◽  
Author(s):  
Naoto Takenoshita ◽  
Raita Fukasawa ◽  
Yusuke Ogawa ◽  
Soichiro Shimizu ◽  
Takahiko Umahara ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Temporal Lobe ◽  
Medial Temporal Lobe ◽  
Neuronal Damage ◽  
Emission Tomography ◽  
Metabolic Abnormalities ◽  
Tau Pathology ◽  
Positron Emission ◽  
The Brain

Background: Type 2 diabetes mellitus (DM) has been shown to increase the risk for cognitive decline and dementia, such as Alzheimer disease (AD) and vascular dementia (VaD). In addition to AD and VaD, there may be a dementia subgroup associated with specific DM-related metabolic abnormalities rather than AD pathology or cerebrovascular disease, referred to as diabetes-related dementia (DrD). Method: We studied 11C-PiB and 11C-PBB3 positron emission tomography (PET) in 31 subjects with DrD and 5 subjects with AD associated with DM to assess amyloid and tau deposits in the brain. Results: All subjects with AD showed both positive PiB and PBB3. However, only 12 out of 31 subjects (39%) with DrD showed positive PiB, whereas 17 out of 21 subjects (81%) who underwent PBB3 PET showed positive PBB3. Depending on the positivity of PiB and PBB3, we classified 21 subjects into a negative PiB and a positive PBB3 pattern (11 cases, 52%), indicating tauopathy, a positive PiB and a positive PBB3 pattern (6 cases, 29%), indicating AD pathology, or a negative PiB and a negative PBB3 pattern (4 cases, 19%). Among 11 subjects showing a negative PiB and a positive PBB3 pattern, there were 2 PBB3 deposit patterns, including the medial temporal lobe only and extensive neocortex beyond the medial temporal lobe. Conclusion: DrD showed variable amyloid and tau accumulation patterns in the brain. DrD may be associated predominantly with tau pathology, in addition to AD pathology and non-amyloid/non-tau neuronal damage due to DM-related metabolic abnormalities.

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