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• Cannabinoid
  ...abinoids are a class of diverse chemical compounds that act on cannabinoid receptors on cells that repress neurotransmitter release in the brain. Ligands for th '''Cannabinoid receptors'''
  20 KB (2,948 words) - 14:51, 27 January 2015
• Tetrahydrocannabinol
  ...c activity, THC appears to result in greater downregulation of cannabinoid receptors than endocannabinoids, further limiting its efficacy over other cannabinoid ...jects is believed to result from activity in the gastro-hypothalamic axis. CB1 activity in the hunger centers in the hypothalamus increases the palatabili
  23 KB (3,443 words) - 11:33, 6 May 2015
• Cannabinol
  ...as a weak agonist of [[CB1 receptors]] but has a higher affinity to [[CB2 receptors]], with lower affinities in comparison to THC.
  1 KB (182 words) - 11:44, 6 May 2015
• JWH-164
  ...qual affinity for the[[ CB1]] and [[CB2 receptor]]s, with a Ki of 6.6nM at CB1 and 6.9nM at CB2. JWH-164 is a positional isomer of the related compound [[
  608 B (93 words) - 07:23, 16 February 2015
• JWH-359
  ...t, with a Ki of 13.0nM and selectivity of around 220x for CB2 over [[CB1]] receptors. It is related to other dibenzopyran CB2 agonists such as [[JWH-133]] and[[
  452 B (75 words) - 07:28, 16 February 2015
• GW-405,833
  ...ith an EC50 of 0.65nM and selectivity of around 1200x for CB2 over [[CB1]] receptors. Animal studies have shown it to possess antiinflammatory and anti-hyperalg
  583 B (89 words) - 07:37, 16 February 2015
• Cannabidiol
  ...N acts as a weak agonist of CB1 receptors but has a higher affinity to CB2 receptors, with lower affinities in comparison to THC. Because it is a somewhat selec
  1,009 B (156 words) - 12:06, 23 February 2015
• Abnormal cannabidiol
  ...GPR55.Further research suggests there are yet more additional cannabinoid receptors.
  1 KB (156 words) - 10:18, 23 February 2015
• Endocannabinoid system
  The endocannabinoid system is a group of neuromodulatory lipids and their receptors in the brain that are involved in a variety of physiological processes incl ...s "[[endocannabinoids]]" and are physiological ligands for the cannabinoid receptors. Endocannabinoids are all eicosanoids.
  25 KB (3,551 words) - 16:53, 23 February 2015
• Effects of cannabis
  '''Cannabinoids and cannabinoid receptors''' ...honuclear neutrophil cells, T8 cells, and T4 cells. In the tonsils the CB2 receptors appear to be restricted to B-lymphocyte-enriched areas.
  34 KB (5,037 words) - 16:49, 23 February 2015
• Cannabis(drug)
  ...g metabolic syndrome risk factors. However, due to the dysphoric effect of CB1 antagonists, this drug is often discontinued due to these side effects. ...nd delta opioid receptors. THC also potentiates the effects of the glycine receptors. The role of these interactions in the "marijuana high" remains elusive.
  33 KB (5,074 words) - 18:47, 29 January 2015
• Cannabis drug testing
  ...y" via activation of neuronal [[cannabinoid]] receptors belonging to the [[CB1]] subtype.
  8 KB (1,224 words) - 12:55, 23 February 2015
• Endocannabinoid
  ...s are substances produced from within the body that activate [[cannabinoid receptors]]. After the discovery of the first cannabinoid receptor in 1988, scientist ...acts as a partial agonist. Anandamide is about as potent as [[THC]] at the CB1 receptor. Anandamide is found in nearly all tissues in a wide range of anim
  6 KB (886 words) - 16:52, 23 February 2015
• Cannabinoid receptor type 1
  The cannabinoid receptor type 1, often abbreviated as CB1, is a G protein-coupled cannabinoid receptor located primarily in the centr ...nly be stable enough to exist in vivo. Recent evidence suggests that these receptors may also possess an allosteric binding site, which may become a target for
  20 KB (2,778 words) - 12:11, 23 February 2015
• CB2 receptor
  ...similarity in amino-acid sequence to the [[cannabinoid receptor type 1]] (CB1) receptor, discovered in 1990. The discovery of this receptor helped provid ...uman CB2 receptor, making it somewhat shorter than the 473-amino-acid-long CB1 receptor.
  11 KB (1,531 words) - 11:55, 23 February 2015
• Cannabinoid receptor antagonist
  ...ists. Cannabidiol, a naturally occurring cannabinoid, is a non-competitive CB1/2 antagonist. ...CB1 receptor represented a new pharmacological target. The first specific CB1 receptor antagonist / inverse agonist was rimonabant, discovered in 1994.
  16 KB (2,402 words) - 12:09, 23 February 2015
• JWH-073
  ...]] and [[CB2]] [[cannabinoid receptors]]. It is somewhat selective for the CB1 subtype, with affinity at this subtype approximately 5x the affinity at CB2 ...found outside the brain, mostly in the immune system. The binding with CB2 receptors has been shown to be similar between JWH-073 and THC.
  2 KB (386 words) - 03:35, 15 February 2015
• JWH-081
  ...] and [[CB2 receptor]]s. With a Ki of 1.2nM it is fairly selective for the CB1 subtype, its affinity at this subtype approximately 10x the affinity at CB2
  413 B (65 words) - 03:37, 15 February 2015
• JWH-019
  ...ds, and may be useful in characterising the active site of the CB1 and CB2 receptors.
  1 KB (212 words) - 03:42, 15 February 2015
• JWH-007
  ...CB1 and 2.94nM at CB2, and JWH-007 displayed optimum binding of 9.50nM at CB1 and 2.94nM at CB2.
  1 KB (220 words) - 03:46, 15 February 2015
• JWH-015
  ...in some model systems can be very potent and efficacious at activating CB1 receptors, and therefore it is not as selective as newer drugs such as [[JWH-133]]. I
  1 KB (202 words) - 03:48, 15 February 2015
• JWH-133
  ...st, with a Ki of 3.4nM and selectivity of around 200x for CB2 over [[CB1]] receptors. It was discovered by, and named after, John W. Huffman. ...antiinflamatory action is induced through agonist action at [[cannabinoid receptors]], which prevents microglial activation that elicits the inflammation. Addi
  1 KB (214 words) - 03:51, 15 February 2015
• KM-233
  ...B2 receptor]]s, with a CB2 affinity of 0.91nM and 13x selectivity over the CB1 receptor. In animal studies it has been found to be effective for the treat
  752 B (118 words) - 03:59, 15 February 2015
• AB-005
  ...e it was reported to have high affinity for both CB1 (Ki = 5.5 nM) and CB2 receptors (Ki = 0.48 nM).[1] AB-005 features groups found in other previously reporte
  1 KB (141 words) - 04:01, 15 February 2015
• JWH-250
  ...]] agonist at both the [[CB1]] and [[CB2 receptor]]s, with a Ki of 11nM at CB1 and 33nM at CB2. Unlike many of the older JWH series compounds, this compou
  1 KB (180 words) - 04:15, 15 February 2015
• SDB-006
  ...ors]], with an EC50 for [[CB1]] activation of 19nM, and 7x selectivity for CB1 over [[CB2]]. It was discovered during research into the related compound [
  353 B (53 words) - 04:27, 15 February 2015
• Cannabinoid receptor type 2
  ...its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provid ...uman CB2 receptor, making it somewhat shorter than the 473-amino-acid-long CB1 receptor.
  11 KB (1,520 words) - 12:12, 23 February 2015
• Cannabis and memory
  == Cannabinoid receptors == ...noid receptor]] research. With the discovery of the endogenous cannabinoid receptors, some recent scientific literature has focused on the effects of phytocanna
  24 KB (3,496 words) - 12:15, 23 February 2015
• Medical cannabis
  ...chers began to study and better understand how cannabinoids acted on these receptors. THC is associated – more than any other cannabinoid – with most of the ...ent of medical cannabis; it is a nonpsychotropic and how it works on brain receptors is not known. CBD represents up to 40% of extracts of Cannabis sativa. A 20
  26 KB (3,891 words) - 14:16, 23 February 2015
• HHC
  ...as later work using more complex compounds such as CP 55,244 to map the [[CB1]] binding site in more detail, but aside from these specific applications,
  2 KB (230 words) - 04:23, 13 February 2015
• HU-243
  ...e [[CB1]] and [[CB2]] receptors, with a binding affinity of 0.041nM at the CB1 receptor, making it marginally more potent than HU-210, which had an affini
  435 B (67 words) - 04:26, 13 February 2015
• Canbisol
  ...nding studies to determine the structure and function of the [[cannabinoid receptors]], but has been made illegal in some countries due to its possible abuse po
  580 B (84 words) - 04:29, 13 February 2015
• HU-210
  ...al stem and progenitor cells likely via a sequential activation of [[CB1]] receptors, Gi/o proteins, and ERK signaling. It was also indicated by this increased ...nti-inflammatory action is induced through the activation of [[cannabinoid receptors]], which prevents microglial activation that elicits the inflammation. In a
  2 KB (328 words) - 06:29, 14 February 2015
• JWH-018
  ...that acts as a full agonist at both the [[CB1]] and [[CB2]] [[cannabinoid receptors]], with some selectivity for CB2. It produces effects in animals similar to ...annabinoid (CB1) receptor five times greater than that of THC. Cannabinoid receptors are found in mammalian brain and spleen tissue; however, the structural det
  9 KB (1,244 words) - 06:53, 14 February 2015
• AM-630
  ...be important in determining affinity and efficacy at both the CB1 and CB2 receptors, and has led to the development of a large number of related derivatives.
  770 B (125 words) - 06:59, 14 February 2015
• WIN 55,212-2
  At 5 µM WIN 55,212-2 inhibit ATP production in sperm in a [[CB1]] receptor-dependent fashion. ...nti-inflammatory action is induced through agonist action at [[cannabinoid receptors]], which prevents microglial activation that elicits the inflammation. Addi
  1 KB (190 words) - 07:06, 14 February 2015
• Pravadoline
  ...lammatory and analgesic drug with an IC50 of 4.9 µM and a Ki of 2511nM at CB1, related in structure to non-steroidal antinflammtory drugs (NSAIDs) such a ...y naloxone (1 mg/kg, s.c.) and pravadoline did not bind to the opioid receptors at concentrations up to 10μM
  2 KB (332 words) - 07:15, 14 February 2015
• A-834,735
  ...ing in compounds that still show significant affinity and efficacy at both receptors despite being CB2 selective overall.
  996 B (137 words) - 07:28, 14 February 2015
• AM-1248
  ...ntoyl group, generally confers significant CB2 selectivity, but reasonable CB1 affinity and selectivity is retained when an N-methylpiperidin-2-ylmethyl s
  803 B (106 words) - 07:38, 14 February 2015
• XLR-11 (drug)
  ...d receptors [[CB1]] and [[CB2]] with a Ki of 24.2nM and a EC50 of 359nM at CB1. It is a 3-(tetramethylcyclopropylmethanoyl)indole derivative related to co
  1 KB (216 words) - 07:46, 14 February 2015
• AB-001
  ...-001 revealed that it acts as a full agonist at CB1 (EC50 = 35 nM) and CB2 receptors (EC50 = 48 nM). However, AB-001 was found to possess only weak cannabimimet
  1 KB (153 words) - 07:52, 14 February 2015
• AM-2233
  ...has been used as its 131I derivative for mapping the distribution of the [[CB1]] receptor in the brain. AM-2233 was found to fully substitute for [[THC]]
  623 B (95 words) - 17:21, 14 February 2015
• SR-144,528
  ...ansferase, an effect that appears to be independent from its action on CB2 receptors.
  695 B (111 words) - 16:36, 14 February 2015
• AB-FUBINACA
  ...nt agonist for the [[cannabinoid receptors]], with Ki values of 0.9nM at [[CB1]] and 23.2nM at[[ CB2]]. It was originally developed by Pfizer in 2009 as a
  700 B (96 words) - 16:44, 14 February 2015
• Rimonabant
  ...ed States. Rimonabant is an inverse agonist for the cannabinoid receptor [[CB1]]. Its main effect is reduction in appetite. Rimonabant was the first selective CB1 receptor blocker to be approved for use anywhere in the world. In Europe, i
  7 KB (947 words) - 16:57, 14 February 2015
• N-(S)-Fenchyl-1-(2-morpholinoethyl)-7-methoxyindole-3-carboxamide
  ...vative has the ratio of affinities reversed however, with a Ki of 8nM at [[CB1]] and 29nM at [[CB2]], which contrasts with the usual trend of 2-methyl der
  1 KB (181 words) - 04:25, 14 April 2015
• Cannabipiperidiethanone
  ...the CB1 and [[CB2 receptor]]s and it was found to have an IC50 of 591nM at CB1 and 968nM at CB2, making it 2.3x and 9.4x weaker than [[JWH-250]] at these
  565 B (81 words) - 17:23, 14 February 2015
• AM-679 (cannabinoid)
  ...inoid]] ligands that are now widely used in research, including the potent CB1 agonists [[AM-694]] and [[AM-2233]], and the selective CB2 agonist [[AM-124
  807 B (122 words) - 17:27, 14 February 2015
• AM-694
  ...1]]. It is used in scientific research for mapping the distribution of CB1 receptors. No public data about AM-694 metabolism is known. AM-694 has already emerge ...iolabelled derivative of AM-694 useful for mapping the distribution of CB1 receptors in the body.
  1 KB (188 words) - 17:30, 14 February 2015
• AM-2201
  ...onist for [[cannabinoid receptors]]. Affinities are: with a Ki of 1.0nM at CB1 and 2.6nM at CB2. The 4-methyl functional analog MAM-2201 probably has simi
  2 KB (301 words) - 17:41, 14 February 2015
• JWH-203
  ...ounds, and has the strongest in vitro binding affinity for the cannabinoid receptors of any compound in the phenylacetyl group. Unexpectedly despite its weaker CB1 Ki in vitro, the 2-methylindole derivative JWH-204 is actually more potent
  1 KB (163 words) - 04:38, 14 April 2015
• APINACA
  ...the [[cannabinoid receptors]], with a Ki of 304.5nM and a EC50 of 585nM at CB1. It had never previously been reported in the scientific or patent literatu
  1 KB (179 words) - 19:21, 14 February 2015
• SDB-001
  ...logical evaluation of SDB-001 revealed that it acts as a full agonist at [[CB1]] (EC50 = 34 nM) and [[CB2 receptor]]s (EC50 = 29 nM). Furthermore, SDB-001
  1 KB (182 words) - 04:32, 14 April 2015
• 9-nor-9β-Hydroxyhexahydrocannabinol
  ...later work using more complex compounds such as[[ CP 55,244]] to map the [[CB1]] binding site in more detail, but aside from these specific applications,
  2 KB (234 words) - 04:31, 14 April 2015
• AM-2232
  ...ective agonist for the [[cannabinoid receptors]], with a Ki of 0.28nM at [[CB1]] and 1.48nM at[[ CB2]].
  259 B (40 words) - 02:48, 15 February 2015
• O-1057
  ...finity for both [[CB1]] and [[CB2 receptors]], with Ki values of 8.36nM at CB1 and 7.95nM at CB2.
  425 B (61 words) - 02:50, 15 February 2015
• O-774
  ...a potent agonist for the [[cannabinoid receptors]], with a Ki of 0.6 nM at CB1, and very potent cannabinoid effects in animal studies.
  251 B (36 words) - 02:52, 15 February 2015
• O-2694
  ...ffinity for both [[CB1]] and [[CB2 receptor]]s, with Ki values of 3.7nM at CB1 and 2.8nM at CB2. However, it has complex pharmacokinetics as most of the a
  692 B (106 words) - 02:56, 15 February 2015
• O-2545
  ...ffinity for both [[CB1]] and [[CB2 receptor]]s, with Ki values of 1.5nM at CB1 and 0.32nM at CB2.
  394 B (60 words) - 02:58, 15 February 2015
• O-2372
  ...ffinity for both [[CB1]] and [[CB2 receptor]]s, with Ki values of 1.3nM at CB1 and 0.57nM at CB2, but is only moderately soluble in water compared to othe
  391 B (63 words) - 03:02, 15 February 2015
• JWH-302
  ...ommon drug JWH-250, though it is slightly less potent with a Ki of 17nM at CB1, compared to 11nM for [[JWH-250]]. Because of their identical molecular wei
  534 B (83 words) - 04:42, 15 February 2015
• EAM-2201
  ...th full agonists and unselectively bind to [[CB1]] and [[CB2]] cannabinoid receptors with low nanomolar affinity.
  2 KB (259 words) - 21:40, 16 February 2015
• JWH-210
  ...(CB1 Ki 0.65nM) respectively, and than the 4-methoxy compound [[JWH-081]] (CB1 Ki 1.2nM). It was discovered by and named after Dr. John W. Huffman. JWH-21
  995 B (150 words) - 12:09, 24 February 2015
• JWH-398
  ...ist at both the[[ CB1]] and [[CB2 receptor]]s. It has mild selectivity for CB1 with a Ki of 2.3nM and 2.8nM at CB2. It was identified by the EMCDDA as an
  477 B (76 words) - 05:30, 15 February 2015
• JWH-424
  ...the 1-propyl homologues in this series showed much lower affinity at both receptors, reflecting a generally reduced affinity for the 8-substituted naphthoylind
  567 B (86 words) - 05:32, 15 February 2015
• JWH-198
  ...ring. It has been used mainly in molecular modelling of the [[cannabinoid receptors]].
  493 B (73 words) - 05:34, 15 February 2015
• List of JWH cannabinoids
  ...ith some selectivity for CB2 with a Ki of 2.9nM ± 2.6 and 9.5nM ± 4.5 at CB1. ...r CB1 is 383nM, meaning that it binds almost 28x more strongly to CB2 than CB1.
  10 KB (1,533 words) - 07:52, 16 February 2015
• JWH-030
  ...cts and is used in scientific research. It is a partial agonist at [[CB1]] receptors, with a Ki of 87nM, making it roughly half the potency of [[THC]]. It was d
  336 B (55 words) - 06:48, 16 February 2015
• JWH-147
  ...r]]s. It is somewhat selective for the CB2 subtype, with a Ki of 11.0nM at CB1 vs 7.1nM at CB2. It was discovered and named after Dr. [[John W. Huffman]].
  510 B (82 words) - 06:50, 16 February 2015
• JWH-307
  ...or]]s. It is somewhat selective for the CB2 subtype, with a Ki of 7.7nM at CB1 vs 3.3nM at CB2. It was discovered by, and named after, Dr. [[John W. Huffm
  432 B (71 words) - 06:52, 16 February 2015
• JWH-098
  ...lindole series tends to increase CB2 affinity, but often at the expense of CB1 binding. JWH-098 is illegal in Russia, Sweden, and the UK, although it is u
  809 B (131 words) - 07:16, 16 February 2015
• Cannabinoid receptor
  Cannabinoid receptors are part of the cannabinoid receptor system in the brain and are involved i [[File:cannabinoid receptors - Weed Depot.jpg|200px|thumb|left|Cannabinoid Receptors]]
  11 KB (1,512 words) - 12:13, 23 February 2015
• List of AM cannabinoids
  *[[AM-087]] — an analgesic CB1 agonist derived from Δ8THC substituted with a side chain on the 3-position *[[AM-251]] — an inverse agonist at the CB1 cannabinoid receptor that is structurally related to SR141716A ([[rimonaban
  6 KB (983 words) - 21:02, 16 February 2015
• CB-13
  ...'' is a [[cannabinoid]] drug, which acts as a potent agonist at both the [[CB1]] and [[CB2 receptor]]s, but has poor blood–brain barrier penetration, an
  475 B (71 words) - 08:09, 16 February 2015
• Tetrahydrocannabinol-C4
  ...or type 1]] and [[cannabinoid receptor type 2]] antagonist, while THC is a CB1 agonist. THC-C4 has rarely been isolated from cannabis samples, but appears
  822 B (124 words) - 21:49, 16 February 2015
• CP 55,940
  A study found that CP 55,940 can upregulate 5-HT2A receptors in mice. CP 55,940 is considered a full agonist at both [[CB1]] and [[CB2]] receptors and has Ki values of 0.58nM and 0.68nM respectively, but is an antagonist a
  1 KB (187 words) - 04:11, 14 April 2015
• Levonantradol
  ...nd analgesic effects via activation of [[CB1]] and [[CB2]] [[cannabinoid]] receptors. Levonantradol is not currently used in medicine as dronabinol or nabilone ...lation of the second messenger, cyclic adenosine monophosphate (cAMP). The CB1 receptor is the most common GPCR in the central nervous system. The activat
  4 KB (555 words) - 04:17, 14 April 2015