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Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens

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Ross, Ruth A, Gibson, T Michael, Brockie, Heather C, Leslie, Mark, Pashmi, Ghazaleh, Craib, Susan J, Di Marzo, Vincenzo, Pertwee, Roger G·2001·British Journal of Pharmacology

DOI 10.1038/sj.bjp.0703850PMC PMC1572597

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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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BackgroundMethodInfluential
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Influential
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Background
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BackgroundInfluential
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“Also, binding of 400 pM [(3)H]-resinferatoxin (RTX, 43 Ci/mmol; Perkin Elmer Life Sciences) to TRPV1 receptors was evaluated by rapid filtration assays, performed as already described.(39) In all experiments, unspecific binding was determined in the presence of 1”
Method
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Background
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BackgroundInfluential
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Background
Anandamide and methanandamide induce both vanilloid VR1- and cannabinoid CB1 receptor-mediated changes in heart rate and blood pressure in anaesthetized rats
Malinowska, B., Kwolek, G., & Göthert, M. (2001) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-001-0498-6 · Cited by 121
“Similarly, the anandamide-induced contractile response of guinea-pig isolated bronchus (Tucker et al. 2001) and ileum (Mang et al. 2001) and the inhibition of the amplitude of electrically evoked contractions in the mouse isolated vas deferens ( Ross et al. 2001 ) are due to activation of VR1 receptors.”
BackgroundResultInfluential
Highly Selective CB1 Cannabinoid Receptor Ligands and Novel CB1/VR1 Vanilloid Receptor “Hybrid” Ligands
Marzo, V. D., Bisogno, T., PETROCELLIS, L. D., Brandi, I., Jefferson, R. G., Winckler, R., Davis, J. B., DASSE, O. A., Mahadevan, A., Razdan, R. K., et al. (2001) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.2001.4354 · Cited by 120
Anandamide Inhibits Nuclear Factor-κB Activation through a Cannabinoid Receptor-Independent Pathway
Sancho, R., Calzado, M. A., Di Marzo, V., Appendino, G., & Muñoz, E. (2003) · Molecular Pharmacology · doi:10.1124/mol.63.2.429 · Cited by 120
“…AEA investigated here were totally inactive on NF- B. Remarkably, D ow nloaded from although arvanil was shown to activate both CB1 and VR1 receptors (Melck et al., 1999a; Ross et al., 2001), some of its biological functions were suggested to be independent of these receptors (Brooks et al., 2002).”
Background
What we know and do not know about the cannabinoid receptor 2 (CB2)
Malfitano, A. M., Basu, S., Maresz, K., Bifulco, M., & Dittel, B. N. (2014) · Seminars in Immunology · doi:10.1016/j.smim.2014.04.002 · Cited by 117
Modulation of anxiety-like behaviour by Transient Receptor Potential Vanilloid Type 1 (TRPV1) channels located in the dorsolateral periaqueductal gray
Terzian, A. L. B., de Aguiar, D. C., Guimarães, F. S., & Moreira, F. A. (2008) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2008.11.004 · Cited by 111
Pharmacological Characterization of the Anandamide Cyclooxygenase Metabolite: Prostaglandin E2 Ethanolamide
Ross, R. A., Craib, S. J., Stevenson, L., Pertwee, R. G., Henderson, A., Toole, J. J., & Ellington, H. C. (2002) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.301.3.900 · Cited by 110
“Kd values for [ 3H]PGE2 and [ 3H]resiniferatoxin binding to EP receptor membranes and VR1 receptor membranes were obtained from Abramovitz et al. (2000) and Ross et al. (2001), respectively.”
BackgroundMethodResultInfluential
Chapter 15 Anandamide and the Vanilloid Receptor (TRPV1)
Tóth, A., Blumberg, P. M., & Boczán, J. (2009) · Vitamins and hormones · doi:10.1016/s0083-6729(09)81015-7 · Cited by 113
Cannabinoids and the Brain
Köfalvi, A. (2007) · Springer eBooks · doi:10.1007/978-0-387-74349-3 · Cited by 110
“Because CB 2 receptors are also expressed by neurons under in vitro conditions (Ross et al., 2001), it is possible that CB 2 receptor expression is induced in “stressed” neurons.”
Background
Lipids as regulators of the activity of transient receptor potential type V1 (TRPV1) channels
PETROCELLIS, L. D., & Marzo, V. D. (2005) · Life Sciences · doi:10.1016/j.lfs.2005.05.021 · Cited by 107
2-AG promotes the expression of conditioned fear via cannabinoid receptor type 1 on GABAergic neurons
Llorente‐Berzal, A., Terzian, A. L. B., Marzo, V. D., Micale, V., Viveros, M., & Wotjak, C. T. (2015) · Psychopharmacology · doi:10.1007/s00213-015-3917-y · Cited by 112
“In fact, behavioral consequences of AM404 seem to result not only indirectly from enhanced CB1 signaling but also directly from activation of TRPV1, since this compound is a potent agonist at this channel too (De Petrocellis et al. 2000; Zygmunt et al. 2000; Ralevic et al. 2001; Ross et al. 2001).”
Background
Local interactions between anandamide, an endocannabinoid, and ibuprofen, a nonsteroidal anti-inflammatory drug, in acute and inflammatory pain
Guindon, J., Léan, A. D., & Beaulieu, P. (2006) · Pain · doi:10.1016/j.pain.2005.12.007 · Cited by 107
“…cannabinoid, is an agonist with a 4-fold selectivity for the CB1 receptor (Ki = 89 nM) over the CB2 receptor (Ki = 371 nM) and was purchased already in a liquid form in water-dispersible emulsion and further dissolved in normal saline (0.9% NaCl in water) (Pertwee et al., 1995; Ross et al., 2001).”
BackgroundInfluential
Binding, degradation and apoptotic activity of stearoylethanolamide in rat C6 glioma cells
Maccarrone, M., Pauselli, R., Rienzo, M. D., & Finazzi‐Agrò, A. (2002) · Biochemical Journal · doi:10.1042/bj20020438 · Cited by 102
Endocannabinoids modulate stress‐induced suppression of hippocampal cell proliferation and activation of defensive behaviours
Hill, M. N., Kambo, J. S., Sun, J. C., Gorzalka, B. B., & Galea, L. A. M. (2006) · European Journal of Neuroscience · doi:10.1111/j.1460-9568.2006.05061.x · Cited by 101
“cannabinoid receptors, endocannabinoids, as well as AM404, are able to activate vanilloid VR1 receptors (Zygmunt et al., 2000; Ross et al., 2001).”
Background
Anxiolytic-like effects induced by blockade of transient receptor potential vanilloid type 1 (TRPV1) channels in the medial prefrontal cortex of rats
de Aguiar, D. C., Terzian, A. L. B., Guimarães, F. S., & Moreira, F. A. (2009) · Psychopharmacology · doi:10.1007/s00213-009-1532-5 · Cited by 101
“The endocannabinoid anandamide act as an “endovanilloid”, although with an affinity around ten times lower than for CB1 (Ross et al. 2001; Smart et al. 2000; Zygmunt et al. 1999).”
Background
Differential role of the hippocampal endocannabinoid system in the memory consolidation and retrieval mechanisms
Alvares, L. D. O., Genro, B. P., Diehl, F., & Quillfeldt, J. A. (2008) · Neurobiology of Learning and Memory · doi:10.1016/j.nlm.2008.01.009 · Cited by 99
Identification of Species-specific Determinants of the Action of the Antagonist Capsazepine and the Agonist PPAHV on TRPV1
Phillips, E., Reeve, A. J., Bevan, S., & McIntyre, P. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m313328200 · Cited by 100
Follicle-Stimulating Hormone Activates Fatty Acid Amide Hydrolase by Protein Kinase A and Aromatase-Dependent Pathways in Mouse Primary Sertoli Cells
Rossi, G., Gasperi, V., Paro, R., Barsacchi, D., Cecconi, S., & Maccarrone, M. (2006) · Endocrinology · doi:10.1210/en.2006-0969 · Cited by 95
Full Inhibition of Spinal FAAH Leads to TRPV1-Mediated Analgesic Effects in Neuropathic Rats and Possible Lipoxygenase-Mediated Remodeling of Anandamide Metabolism
Starowicz, K., Makuch, W., Korostyński, M., Małek, N., Ślęzak, M., Żychowska, M., Petrosino, S., PETROCELLIS, L. D., Cristino, L., Przewłocka, B., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0060040 · Cited by 97
“channel by AEA have been thoroughly studied [9,10,11].”
Background
Involvement of endocannabinoids in antidepressant and anti-compulsive effect of fluoxetine in mice
Umathe, S. N., Manna, S. S. S., & Jain, N. S. (2011) · Behavioural Brain Research · doi:10.1016/j.bbr.2011.04.031 · Cited by 98
Cannabinoid Agonists but not Inhibitors of Endogenous Cannabinoid Transport or Metabolism Enhance the Reinforcing Efficacy of Heroin in Rats
Solinas, M., Panlilio, L. V., Tanda, G., Makriyannis, A., Matthews, S. A., & Goldberg, S. R. (2005) · Neuropsychopharmacology · doi:10.1038/sj.npp.1300754 · Cited by 103
Anatomical Distribution of Receptors, Ligands and Enzymes in the Brain and in the Spinal Cord: Circuitries and Neurochemistry
Marsicano, G., & Kuner, R. (2007) · Springer eBooks · doi:10.1007/978-0-387-74349-3_10 · Cited by 103
“Because CB 2 receptors are also expressed by neurons under in vitro conditions (Ross et al., 2001), it is possible that CB 2 receptor expression is induced in “stressed” neurons.”
Background
Antihyperalgesic effects of local injections of anandamide, ibuprofen, rofecoxib and their combinations in a model of neuropathic pain
Guindon, J., & Beaulieu, P. (2006) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.12.002 · Cited by 90
Cannabinoid CB2 Receptor-Mediated Anti-nociception in Models of Acute and Chronic Pain
Jhaveri, M. D., Sagar, D. R., Elmes, S. J. R., Kendall, D. A., & Chapman, V. (2007) · Molecular Neurobiology · doi:10.1007/s12035-007-8007-7 · Cited by 89
A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea‐pig bronchus
Craib, S. J., Ellington, H. C., Pertwee, R. G., & Ross, R. A. (2001) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0704223 · Cited by 88
“KB values for capsazepine and its 95% con®dence limits were determined by symmetrical (2+2) dose parallel line assays (see Ross et al., 2001).”
BackgroundMethodInfluential
Endocannabinoid-mediated modulation of stress responses: Physiological and pathophysiological significance
Finn, D. P. (2009) · Immunobiology · doi:10.1016/j.imbio.2009.05.011 · Cited by 91
“Caution should be exercised when attributing the effects of anandamide, or drugs which increase its availability, to CB1 receptors, since anandamide (and indeed AM404) has direct agonistic activity at the vanilloid receptor TRPV1 (De Petrocellis et al., 2000; De Petrocellis et al., 2001; Di Marzo et al., 2001; Ross et…”
Influential
Neuropathic pain and the endocannabinoid system in the dorsal raphe: pharmacological treatment and interactions with the serotonergic system
Palazzo, E., De Novellis, V., Petrosino, S., Marabese, I., Vita, D., Giordano, C., Di Marzo, V., Mangoni, G. S., Rossi, F., & Maione, S. (2006) · European Journal of Neuroscience · doi:10.1111/j.1460-9568.2006.05086.x · Cited by 86
A-kinase anchoring protein 150 controls protein kinase C-mediated phosphorylation and sensitization of TRPV1
Jeske, N. A., Patwardhan, A. M., Ruparel, N. B., Akopian, A. N., Shapiro, M. S., & Henry, M. A. (2009) · Pain · doi:10.1016/j.pain.2009.08.002 · Cited by 84
“9) [32], and certain cannabinoids [27,29] to stimulate neuronal activation and nociception [7].”
Background
Actions and Regulation of Ionotropic Cannabinoid Receptors
PETROCELLIS, L. D., Nabissi, M., Santoni, G., & Ligresti, A. (2017) · Advances in pharmacology · doi:10.1016/bs.apha.2017.04.001 · Cited by 81
Arvanil-induced inhibition of spasticity and persistent pain: evidence for therapeutic sites of action different from the vanilloid VR1 receptor and cannabinoid CB1/CB2 receptors
Brooks, J. W., Pryce, G., Bisogno, T., Jaggar, S., Hankey, D. J. R., Brown, P., Bridges, D., Ledent, C. A., Bifulco, M., Rice, A. S. C., et al. (2002) · European Journal of Pharmacology · doi:10.1016/s0014-2999(02)01369-9 · Cited by 81
Cannabinoid-based drugs targeting CB1 and TRPV1, the sympathetic nervous system, and arthritis
Lowin, T., & Straub, R. H. (2015) · Arthritis Research & Therapy · doi:10.1186/s13075-015-0743-x · Cited by 82
“ent capsaicin, although it does not activate the receptor like capsaicin [56].”
Background
Anandamide is a partial agonist at native vanilloid receptors in acutely isolated mouse trigeminal sensory neurons
Roberts, L. A., Christie, M. J., & Connor, M. A. (2002) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0704904 · Cited by 79
“Another study compared radioligand binding and 45Ca2+- uptake in CHO cells transfected with rat VR1 and concluded that AEA and AM404 were low potency, low e cacy VR1 agonists, despite AEA and AM404 producing a similar maximal 45Ca2+-uptake to capsaicin and resiniferatoxin (Ross et al., 2001).”
Background
The effect of cannabinoids on capsaicin-evoked calcitonin gene-related peptide (CGRP) release from the isolated paw skin of diabetic and non-diabetic rats
Ellington, H. C., Cotter, M. A., Cameron, N. E., & Ross, R. A. (2002) · Neuropharmacology · doi:10.1016/s0028-3908(02)00040-0 · Cited by 79
Involvement of transient receptor potential vanilloid type 1 channels in the pro-convulsant effect of anandamide in pentylenetetrazole-induced seizures
Manna, S. S. S., & Umathe, S. N. (2012) · Epilepsy Research · doi:10.1016/j.eplepsyres.2012.02.003 · Cited by 77
Anandamide induces cough in conscious guinea‐pigs through VR1 receptors
Jia, Y., McLeod, R. L., Wang, X., Parra, L. E., Egan, R. W., & Hey, J. A. (2002) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0704950 · Cited by 77
“Anandamide has been shown, using displacement and binding studies, to bind to the same site on VR1 as capsaicin (Ross et al., 2001), which is in the intracellular region of cell membrane (Jung et al., 1999).”
Method
Human adipose tissue binds and metabolizes the endocannabinoids anandamide and 2-arachidonoylglycerol
Spoto, B., Fezza, F., Parlongo, G., Battista, N., Sgro, E., Gasperi, V., Zoccali, C., & Maccarrone, M. (2006) · Biochimie · doi:10.1016/j.biochi.2006.07.019 · Cited by 75
6ʺ-Azidohex-2ʺ-yne-cannabidiol: a potential neutral, competitive cannabinoid CB1 receptor antagonist
Thomas, A., Ross, R. A., Saha, B., Mahadevan, A., Razdan, R. K., & Pertwee, R. G. (2004) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2004.01.023 · Cited by 76
Cholesterol‐dependent modulation of type 1 cannabinoid receptors in nerve cells
Bari, M., Paradisi, A., Pasquariello, N., & Maccarrone, M. (2005) · Journal of Neuroscience Research · doi:10.1002/jnr.20546 · Cited by 75
“In all binding experiments, nonspecific binding was determined in the presence of 1 mM ‘‘cold’’ agonist (Maccarrone et al., 2000a; Ross et al., 2001).”
BackgroundMethodInfluential
Spinal anandamide produces analgesia in neuropathic rats: Possible CB1- and TRPV1-mediated mechanisms
Starowicz, K., Makuch, W., Osikowicz, M., Piscitelli, F., Petrosino, S., Marzo, V. D., & Przewłocka, B. (2011) · Neuropharmacology · doi:10.1016/j.neuropharm.2011.11.021 · Cited by 78
CB1 and CB2 Cannabinoid Receptor Agonists Induce Peripheral Antinociception by Activation of the Endogenous Noradrenergic System
Romero, T. R. L., Resende, L. C., Guzzo, L. S., & Duarte, I. D. G. (2013) · Anesthesia & Analgesia · doi:10.1213/ane.0b013e3182707859 · Cited by 74
Evaluation of the emotional phenotype and serotonergic neurotransmission of fatty acid amide hydrolase-deficient mice
Cassano, T., Gaetani, S., Macheda, T., Laconca, L., Romano, A., Morgese, M. G., Cimmino, C. S., Chiarotti, F., Bambico, F. R., Gobbi, G., et al. (2011) · Psychopharmacology · doi:10.1007/s00213-010-2051-0 · Cited by 72
“Anandamide has very low affinity and potency at TRPV1 compared to CB1 receptors (Ross et al. 2001) and has a short intracellular half-life due to the rapid enzymatic hydrolysis, mostly catalysed by FAAH (Piomelli 2003).”
Phosphorylation-Dependent Desensitization by Anandamide of Vanilloid Receptor-1 (TRPV1) Function in Rat Skeletal Muscle Arterioles and in Chinese Hamster Ovary Cells Expressing TRPV1
Lizanecz, E., Bagi, Z. A., Pásztor, E. T., Papp, Z. L., Edes, I. F., Kedei, N., Blumberg, P. M., & Tóth, A. (2005) · Molecular Pharmacology · doi:10.1124/mol.105.015644 · Cited by 70
“Ross et al. (2001) reported only low efficacy of anandamide at TRPV1 receptors overexpressed in CHO cells, which was greatly enhanced by inhibition of fatty acid amide hydrolase.”
BackgroundResultInfluential
Effect of Lipid Rafts on Cb2 Receptor Signaling and 2-Arachidonoyl-Glycerol Metabolism in Human Immune Cells
Bari, M., Spagnuolo, P., Fezza, F., Oddi, S., Pasquariello, N., Finazzi‐Agrò, A., & Maccarrone, M. (2006) · The Journal of Immunology · doi:10.4049/jimmunol.177.8.4971 · Cited by 69
“Also the binding of 200 pM [(3)H]RTX was evaluated by rapid filtration assays, performed as reported previously (49).”
BackgroundMethodInfluential
Anandamide activates peripheral nociceptors in normal and arthritic rat knee joints
Gauldie, S. D., McQueen, D. S., Pertwee, R. G., & Chessell, I. P. (2001) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0703890 · Cited by 70
“…on the VR1 receptor has been demonstrated using transfected human receptors (Smart et al., 2000), on sensory nerves controlling vasodilatation in isolated arteries (Zygmunt et al., 1999), and the amplitude of electrically-evoked contractions in the mouse isolated vas deferens (Ross et al., 2001).”
Background
Impaired endocannabinoid signalling in the rostral ventromedial medulla underpins genotype-dependent hyper-responsivity to noxious stimuli
Rea, K., Olango, W. M., Okine, B. N., Madasu, M. K., McGuire, I. C., Coyle, K., Harhen, B., Roche, M., & Finn, D. P. (2013) · Pain · doi:10.1016/j.pain.2013.09.012 · Cited by 69
“In addition to activating CB1 receptors, AEA is also an agonist at the transient receptor potential vanilloid subtype 1 (TRPV1) channel [13,16,74,79], the expression of which has been reported in the RVM [80].”
Background
Inhibitory effect of ginger (Zingiber officinale) on rat ileal motility in vitro
Borrelli, F., Capasso, R., Pinto, A., & Izzo, A. A. (2004) · Life Sciences · doi:10.1016/j.lfs.2003.10.023 · Cited by 69
Halogenation of a capsaicin analogue leads to novel vanilloid TRPV1 receptor antagonists
Appendino, G., Harrison, S., PETROCELLIS, L. D., Daddario, N., Bianchi, F., Moriello, A. S., Trevisani, M., Benvenuti, F., Geppetti, P., & Marzo, V. D. (2003) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0705387 · Cited by 69
“…assays carried out with membranes (50 mg per tube) from HEK cells overexpressing the receptors, prepared as described previously (Ross et al., 2001), and the highaffinity TRPV1 ligand RTX (48Cimmol 1, NEN-Dupont), using the incubation conditions described previously (Ross et al., 2001).”
Method
Cellular transport of anandamide, 2-arachidonoylglycerol and palmitoylethanolamide—targets for drug development?
Fowler, C. J., & Jacobsson, S. O. P. (2002) · Prostaglandins Leukotrienes and Essential Fatty Acids · doi:10.1054/plef.2001.0357 · Cited by 69
Intraplantar injection of anandamide inhibits mechanically-evoked responses of spinal neurones via activation of CB2 receptors in anaesthetised rats
Sokal, D. M., Elmes, S. J. R., Kendall, D. A., & Chapman, V. (2003) · Neuropharmacology · doi:10.1016/s0028-3908(03)00195-3 · Cited by 67
Endocannabinoids mediate neuroprotection after transient focal cerebral ischemia
Schomacher, M., Müller, H. D., Sommer, C., Schwab, S., & Schäbitz, W. (2008) · Brain Research · doi:10.1016/j.brainres.2008.09.019 · Cited by 65

Authors: Ross, R. A., Gibson, T. M., Brockie, H. C., Leslie, M., Pashmi, G., Craib, S. J., Di Marzo, V., & Pertwee, R. G.
Affiliations: University of Aberdeen (GB)
Corresponding author: Ross, Ruth A
ORCID: Ross, Ruth A
Pertwee, Roger G
Venue: British Journal of Pharmacology
Publisher: Wiley
Published: 2001-02
Volume: 132
Issue: 3
Pages: 631-640
ISSN: 0007-1188 (ISSN-L)
1476-5381
DOI: 10.1038/sj.bjp.0703850
PMC: PMC1572597
OpenAlex: W2021876302
Cited by: 237
References: 28
Citations by year: 2026: 3 · 2025: 1 · 2024: 6 · 2023: 2 · 2022: 1 · 2021: 1 · 2020: 4 · 2019: 2 · 2018: 6 · 2017: 8 · 2016: 4 · 2015: 12 · 2014: 6 · 2013: 12 · 2012: 6
FWCI: 9.89
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor, 2919 d)
Locations: British Journal of Pharmacology (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: Wellcome Trust
National Institute on Drug Abuse (P01DA009789, DA 09789)
Topics: Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Physiology (medical) › Pain Mechanisms and Treatments
Keywords: anandamide, structure-activity relationship, vanilloid receptor 1, CB1 receptor, cannabinoid analogues, AM404, resiniferatoxin, capsaicin, vas deferens contraction, SR141716A, capsazepine, methanandamide, receptor binding affinity
MeSH terms: Rimonabant, Animals, Arachidonic Acids, Binding, Competitive, Biological Transport, Calcium, Calcium Channel Blockers, Cannabinoids, Capsaicin, Drug Interactions, Electric Stimulation, Enzyme Inhibitors, Cricetinae, Male, Morpholines, Muscle Contraction, Naphthalenes, Phenylmethylsulfonyl Fluoride, Piperidines, Pyrazoles, Radioligand Assay, Receptors, Drug, Structure-Activity Relationship, Transfection, Vas Deferens, CHO Cells, Receptors, Cannabinoid, Benzoxazines, TRPV Cation Channels, Mice, Polyunsaturated Alkamides, Endocannabinoids

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Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens

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