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*  MN-25
CANNABINOID RECEPTOR MODULATORS, THEIR PROCESSES OF PREPARATION, AND USE OF CANNABINOID RECEPTOR MODULATORS IN TREATING ... C3 AMIDO-INDOLE CANNABINOID RECEPTOR MODULATORS. Bioorganic and Medical Chemistry Letters. Volume 12 issue 17, 2 September 2002 ... 2002). "C-3 Amido-Indole cannabinoid receptor modulators". Bioorganic & Medicinal Chemistry Letters. 12 (17): 2399-402. doi: ... that acts as a reasonably selective agonist of peripheral cannabinoid receptors. It has moderate affinity for CB2 receptors ...
*  RVD-Hpα
It is shown that pepcan-12 opposite acts as a potent CB2 cannabinoid receptor positive allosteric modulator (PAM). RVD-Hpα also ... shown to act as negative allosteric modulators (NAM) of cannabinoid CB1 receptors. ... Recently it was shown that RVD-Hpα (also called Pepcan-12) is a potent negative allosteric modulator at CB1 receptors, together ... is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage". ...
*  AM-630
September 2002). "C-3 Amido-indole cannabinoid receptor modulators". Bioorganic & Medicinal Chemistry Letters. 12 (17): 2399- ... AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2, with ... May 2010). "Brain cannabinoid CB2 receptor in schizophrenia". Biological Psychiatry. 67 (10): 974-82. doi:10.1016/j.biopsych. ... February 1999). "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630 ...
*  GAT100
... is a negative allosteric modulator of the cannabinoid CB1 receptor. Org 27569 PSNCBAM-1 ZCZ-011 Pushkar M. Kulkarni; ... "Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, ... "Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s)". Journal of ...
*  ZCZ-011
... is a positive allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 PSNCBAM-1 Justin L. Poklis; ... "A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects". ... A Novel Pharmacological Tool for Investigation of the Cannabinoid Receptor in Mouse Brain Using Clean Screen FASt™ Column ...
*  PSNCBAM-1
... is a negative allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 ZCZ-011 German N, Decker AM, ... "Diarylureas as Allosteric Modulators of the Cannabinoid CB1 Receptor: Structure-Activity Relationship Studies on 1-(4- ... a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats". British Journal of Pharmacology. ...
*  RTI-371
Computational study of RTI-371, a positive allosteric modulator of the cannabinoid CB1 receptor. MSc Thesis, 2011, The ... when it was discovered that RTI-371 also acts as a positive allosteric modulator of the hCB1 human cannabinoid receptor. List ... Positive allosteric modulation of the human cannabinoid (CB) receptor by RTI-371, a selective inhibitor of the dopamine ... It may be caused by lack of BBB penetration, or interactions at alternative receptor sites. Recently the second of these ...
*  Cannabinoid receptor antagonist
"Are cannabidiol and Δ9-tetrahydrocannabivarin negative modulators of the endocannabinoid system? A systematic review". British ... cannabinoid receptor 1 (CB1) and 2 (CB2). Both receptors are 7-transmembrane G-protein coupled receptors (GPCRs) which inhibit ... A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of ... The endogenous cannabinoid system includes cannabinoid receptors, their endogenous ligands (endocannabinoids) and enzymes for ...
*  Cannabinoid receptor type 1
Nickols HH, Conn PJ (January 2014). "Development of allosteric modulators of GPCRs for treatment of CNS disorders". ... Discovery and development of Cannabinoid Receptor 1 Antagonists Cannabinoid receptor Cannabinoid receptor type 2 (CB2) GRCh38: ... The cannabinoid type 1 receptor, often abbreviated as CB1, is a G protein-coupled cannabinoid receptor located primarily in the ... Selective CB1 agonists may be used to isolate the effects of the receptor from the CB2 receptor, as most cannabinoids and ...
*  Org 27569
... is a drug which acts as a potent and selective positive allosteric modulator of the cannabinoid CB1 receptor. Studies ... "Allosteric modulation of the cannabinoid CB1 receptor". Molecular Pharmacology. 68 (5): 1484-95. doi:10.1124/mol.105.016162. ... However while Org 27569 increases the ability of CB1 agonists to bind to the receptor, it decreases their efficacy at ... in vitro suggest that it binds to a regulatory site on the CB1 receptor target, causing a conformational change that increases ...
*  List of investigational analgesics
... cannabinoid receptor modulator[39] CMX-020 - TRPV1 modulator as well as CB1 and CB2 receptor modulator[40] Dronabinol (Δ9-THC; ... CB2 receptor agonist[36] Cannabidiol (CBD) - cannabinoid receptor modulator[37][38] Cannabidivarin (CBDV; GWP-42006) - ... non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid receptor partial agonist[ ... TRPV1 modulator as well as CB1 and CB2 receptor modulator[25] DWP-05195 (TR-1) - TRPV1 antagonist[26] GRC-6211 - TRPV1 agonist[ ...
*  Thujone
... is a GABAA receptor antagonist and more specifically, a GABAA receptor positive allosteric modulator. By inhibiting ... ISBN 0-8118-1650-8 p. 152 Meschler JP, Howlett AC (March 1999). "Thujone exhibits low affinity for cannabinoid receptors but ... for many years thujone was thought to act similarly to THC on the cannabinoid receptors; however, this has since been proven ... Modulation of Ionotropic GABA Receptors by Natural Products of Plant Origin Dettling A, Grass H, Schuff A, Skopp G, Strohbeck- ...
*  Cannabidiol
... wrongly mention agonist action of CBD on cannabinoid receptors while the English version says CBD is a cannabinoid receptor ... It is an allosteric modulator of the μ- and δ-opioid receptors as well. Cannabidiol's pharmacological effects have additionally ... "The orphan receptor GPR55 is a novel cannabinoid receptor". British Journal of Pharmacology. 152 (7): 1092-101. doi:10.1038/sj. ... a G protein-coupled receptor and putative cannabinoid receptor that is expressed in the caudate nucleus and putamen in the ...
*  List of investigational antipsychotics
... cannabinoid receptor modulator, antioxidant, other actions[18][19] Basmisanil (RG-1662, RO-5186582) - GABAA receptor α5 subunit ... NMDA receptor glycine-site positive allosteric modulator[13] PF-4958242 - AMPA receptor positive allosteric modulator[14] ... 5-HT6 receptor antagonist[2] F-17464 - D3 receptor antagonist, 5-HT1A receptor partial agonist, and weak D2 receptor partial ... cannabinoid receptor modulator (phytocannabinoid-based chewing gum)[17] Cannabidiol (CBD; GW-42003, GWP-42003, GWP-42003-P, ECP ...
*  Tetrahydrocannabinol
... as the drug has a relatively low cannabinoid receptor efficacy and affinity. In populations of low cannabinoid receptor density ... is a positive allosteric modulator of the μ- and δ-opioid receptors. Due to its partial agonistic activity, THC appears to ... The actions of THC result from its partial agonist activity at the cannabinoid receptor CB1 (Ki=10nM), located mainly in the ... The psychoactive effects of THC are primarily mediated by the activation of cannabinoid receptors, which result in a decrease ...
*  Entourage effect
Cannabinoid system modulators like N-palmitoylethanolamine may be said to exhibit the entourage effect, increasing receptors ... Other cannabinoids', terpenoids', and flavonoids' contribution to clinical cannabis effects has been espoused as an "entourage ... Fine PG, Rosenfeld MJ (2013-10-29). "The endocannabinoid system, cannabinoids, and pain". Rambam Maimonides Medical Journal. 4 ... This entourage effect may represent a novel endogenous cannabinoid activity molecular regulation route. ...
*  Psychoneuroimmunology
For example, SSRIs, SNRIs and tricyclic antidepressants acting on serotonin, norepinephrine, dopamine and cannabinoid receptors ... Glutamate agonists, cytokine inhibitors, vanilloid-receptor agonists, catecholamine modulators, ion-channel blockers, ... by which cannabinoid CB1 receptors modulate the excitability of dorsal raphe serotonin neurons. Data suggest that the ... acetylcholine modulators, melatonin analogs (such as Ramelton), adenosine receptor antagonists and several miscellaneous drugs ...
*  Cachexia
... and ghrelin receptor agonist Anabolic catabolic transforming agents such as MT-102 Selective androgen receptor modulators ... Thalidomide and cytokine antagonists Cannabinoids Omega-3 fatty acids, including eicosapentaenoic acid (EPA) Non-steroidal anti ... NF-κB is a known regulator of the genes that encode cytokines, and cytokine receptors. The increased production of cytokines ...
*  Agonist
... or selective receptor modulators. Potency is the amount of agonist needed to elicit a desired response. The potency of an ... An example is the cannabinoid inverse agonist rimonabant. A superagonist is a term used by some to identify a compound that is ... An inverse agonist is an agent that binds to the same receptor binding-site as an agonist for that receptor and inhibits the ... Full agonists bind to and activate a receptor with the maximum response that an agonist can elicit at the receptor. One example ...
*  Receptor (biochemistry)
... which are believed to relate to the inhibition of the constitutive activity of the cannabinoid receptor. Mutations in receptors ... Allosteric modulators: They do not bind to the agonist-binding site of the receptor but instead on specific allosteric binding ... receptors, G protein-linked (metabotropic) hormone receptors, and enzyme-linked hormone receptors. Intracellular receptors are ... The insulin receptor is an example. Type 4: Nuclear receptors - While they are called nuclear receptors, they are actually ...
*  Autopharmacology
... transmitters and modulators involved in their complex response at molecular and cellular level. The control and regulation ... were discovered to exist in the brain and have specific receptors in it, by investigations on the mechanism of action of ... Endorphins Dynorphin Bradykinin Prostaglandins Angiotensin Secretin Gastrin Cholecystokinin Histamine Cannabinoids Substance P ... The main scientific criterion for an autopharmacological agent is the discovery of specific membrane receptors for it and, ...
*  Alpha-7 nicotinic receptor
2007). "Nootropic α7 nicotinic receptor allosteric modulator derived from GABA A receptor modulators". PNAS. 104 (19): 8059- ... "Additive Effects of Endogenous Cannabinoid Anandamide and Ethanol on α7-Nicotinic Acetylcholine Receptor-Mediated Responses in ... The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor implicated in long ... α7 subtype preferring blocker α3β2-Nicotinic receptor α3β4-Nicotinic receptor α4β2-Nicotinic receptor RIC3, a chaperone protein ...
*  Metabolic syndrome
Hotamisligil GS (June 1999). "The role of TNFalpha and TNF receptors in obesity and insulin resistance". Journal of Internal ... Turcotte C, Chouinard F, Lefebvre JS, Flamand N (June 2015). "Regulation of inflammation by cannabinoids, the endocannabinoids ... signaling system plays a critical role in motivational homeostasis as a conduit for reward stimuli and a positive modulator of ... Endocannabinoid-system hyperactivity through CB1 receptor transmission is considered contributory to a range of appetitive ...
*  List of designer drugs
Selective androgen receptor modulators (SARMs) are a novel class of androgen receptor ligands. They are intended to maintain ... Indole containing cannabinoid receptor agonists include: 4-HTMPIPO 5C-MN-24, 5C-NNEI 5F-AB-PICA 5F-ADBICA 5F-AMB-PICA, I-AMB, ... Kanno Y, Ota R, Someya K, Kusakabe T, Kato K, Inouye Y (2013). "Selective androgen receptor modulator, YK11, regulates myogenic ... Zhang X, Sui Z (2013). "Deciphering the selective androgen receptor modulators paradigm". Expert Opin Drug Discov. 8 (2): 191- ...
*  Lipoxin
Russell R, Gori I, Pellegrini C, Kumar R, Achtari C, Canny GO (Dec 2011). "Lipoxin A4 is a novel estrogen receptor modulator". ... It is found that the anti-inflammatory lipid lipoxin A4 is an endogenous allosteric enhancer of the CB1 cannabinoid receptor. ... FPR2, which is now termed the ALX, ALX/FPR, or ALX/FPR2 receptor, is a G protein coupled receptor initially identified as a ... LXA4 and 15-epi-LXA4 are high affinity receptor ligands for and activators of the FPR2 receptor. ...
*  Raymond C. Stevens
2016: The marijuana receptor-human Cannabinoid receptor type 1 (CB1) and the human C-C chemokine receptor type 2 (CCR2) In ... Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator Science 344: 58-64 C. Wang, H. ... 2013: Serotonin receptors 5-HT1B and 5-HT2B, the second HIV co-receptor, C-C chemokine receptor type 5 (CCR5) and the first ... In 2010, the structures of the human chemokine CXCR4 receptor (HIV co-receptor), the human dopamine D3 receptor and the human ...