ArticleBritish journal of pharmacology2001
Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 63 papers.
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Who cites it
63 citing papers in PubMed, 235 citations in OpenAlex.
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- Cannabinoids in neuropathic pain treatment: pharmacological insights and clinical outcomes from recent trials.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
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- Inhibition of Adult Neurogenesis in Male Mice after Repeated Exposure to Paracetamol Overdose.International journal of molecular sciences · 2024Article
- Assessment of clinical outcomes in patients with fibromyalgia: Analysis from the UK Medical Cannabis Registry.Brain and behavior · 2023Article
- Blockade of the endovanilloid receptor, TRPV1, and of the endocannabinoid enzyme, FAAH, within the nucleus accumbens shell elicits anxiolytic-like effects in male rats.Neuroscience letters · 2020Article
- Targeting the endocannabinoid system: a predictive, preventive, and personalized medicine-directed approach to the management of brain pathologies.The EPMA journal · 2020Review
- Modification of TRPV4 activity by acetaminophen.Heliyon · 2020Article
- The prefrontal cortical endocannabinoid system modulates fear-pain interactions in a subregion-specific manner.British journal of pharmacology · 2019Article
- A TRPV1-to-secretagogin regulatory axis controls pancreatic β-cell survival by modulating protein turnover.The EMBO journal · 2017Article
- Blockade of Cannabinoid CB1 Receptors in the Dorsal Periaqueductal Gray Unmasks the Antinociceptive Effect of Local Injections of Anandamide in Mice.Frontiers in pharmacology · 2017Article
- A pro-nociceptive phenotype unmasked in mice lacking fatty-acid amide hydrolase.Molecular pain · 2016Article
- Endovanilloids are potential activators of the trigeminovascular nocisensor complex.The journal of headache and pain · 2016Article
- Cannabinoid-based drugs targeting CB1 and TRPV1, the sympathetic nervous system, and arthritis.Arthritis research & therapy · 2015Review
- 2-AG promotes the expression of conditioned fear via cannabinoid receptor type 1 on GABAergic neurons.Psychopharmacology · 2015Article
- The Endocannabinoid Signaling System in the CNS: A Primer.International review of neurobiology · 2015Review
- Article
- Cocaine-induced endocannabinoid release modulates behavioral and neurochemical sensitization in mice.Addiction biology · 2015Article
- What we know and do not know about the cannabinoid receptor 2 (CB2).Seminars in immunology · 2014Review
- Differential modulation of nociceptive versus non-nociceptive synapses by endocannabinoids.Molecular pain · 2013Article
3 more citing papers are in PubMed but not listed here.
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Authors and funding
8 authors at 3 institutions in 3 countries.
Funding
Abstract
1. This study was directed at exploring the structure-activity relationship for anandamide and certain of its analogues at the rat VR1 receptor in transfected cells and at investigating the relative extent to which anandamide interacts with CB(1) and vanilloid receptors in the mouse vas deferens. 2. pK(i) values for displacement of [(3)H]-resiniferatoxin from membranes of rVR1 transfected CHO cells were significantly less for anandamide (5.78) than for its structural analogues N-(4-hydroxyphenyl)-arachidonylamide (AM404; 6.18) and N-(3-methoxy-4-hydroxy)benzyl-arachidonylamide (arvanil; 6.77). 3. pEC(50) values for stimulating (45)Ca(2+) uptake into rVR1 transfected CHO cells were significantly less for anandamide (5.80) than for AM404 (6.32) or arvanil (9.29). Arvanil was also significantly more potent than capsaicin (pEC(50)=7.37), a compound with the same substituted benzyl polar head group as arvanil. 4. In the mouse vas deferens, resiniferatoxin was 218 times more potent than capsaicin as an inhibitor of electrically-evoked contractions. Both drugs were antagonized to a similar extent by capsazepine (pK(B)=6.93 and 7.18 respectively) but were not antagonized by SR141716A (1 microM). Anandamide was less susceptible than capsaicin to antagonism by capsazepine (pK(B)=6.02) and less susceptible to antagonism by SR141716A (pK(B)=8.66) than methanandamide (pK(B)=9.56). WIN55212 was antagonized by SR141716A (pK(B)=9.02) but not by capsazepine (10 microM). 5. In conclusion, anandamide and certain of its analogues have affinity and efficacy at the rat VR1 receptor. In the mouse vas deferens, which seems to express vanilloid and CB(1) receptors, both receptor types appear to contribute to anandamide-induced inhibition of evoked contractions.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.