Cannabinoids

<p>GW842166X: Potent CB2 agonist, EC50=63 nM, inactive at CB1, in Phase 2 trials.</p>

<p>AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.</p>

<p>Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also</p>

<p>Yangonin (Y100550) is a novel CB1 receptor ligand with affinity for human recombinant CB1 receptors.</p>

<p>(±)-Ibipinabant ((±)-SLV319) has been used in trials studying the treatment of Obesity and Obesity and Type 2 Diabetes.</p>

<p>Voacamine: an indole alkaloid, CB1 antagonist, inhibits P-gp, may affect rhythm.</p>

<p>CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.</p>

<p>A-836339: Potent cannabinoid, CB2-focused (Ki=0.64nM), lesser CB1 affinity (Ki=270nM); analgesic, anti-inflammatory in mice.</p>

<p>LY2828360: CB2 agonist, Ki=40.3 nM; biases CB2 over CB1 with EC50s of 20.1 nM and &gt;100 μM.</p>

<p>Olivetol, found in lichens, is an organic antioxidant and THC synthesis precursor.</p>

<p>Otenabant (CP-945598) has been investigated for the treatment of Obesity.</p>

<p>Linoleoyl Ethanolamide is an endocannabinoid agent.</p>

<p>CID 16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.</p>

<p>N-Oleoyl glycine, a lipoamino acid, was able to promote 3T3-L1 adipogenesis through the activation of CB1 receptor and the enhancement of insulin-mediated Akt</p>

<p>Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM).</p>

<p>ML-191 is an inhibitor of LPI-induced phosphorylation of ERK1/2.</p>

<p>AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.</p>

<p>ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with EC50 of 0.26 μM.</p>

<p>AM251: potent CB1 blocker (IC50: 8 nM), 306x CB2 selective; GPR55 activator (EC50: 39 nM).</p>

<p>PSB-SB-487 is antagonist of GPR55.</p>

<p>BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体，其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki&gt; 2 μM)。</p>

<p>GW 405833 (L-768242) is an agonist of cannabinoid-2 (CB(2)) receptor-selective</p>

<p>ARN272 is a FAAH-like anandamide transporter (FLAT) inhibitor (IC50: 1.8 μM).</p>

<p>Hemopressin: Nonapeptide, α1-hemoglobin derivative, CB1 inverse agonist, isolated from rats, oral, reduces inflammatory pain.</p>

<p>Hemopressin is a nonapeptide, CB2 agonist, derived from rat hemoglobin, with antinociceptive properties.</p>

<p>RVD-Hpα acetate is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist.</p>

<p>Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).</p>

<p>TM38837 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.</p>

<p>Tetrahydromagnolol can activate cannabinoid (CB) receptors.</p>

<p>ML-193: GPR55 antagonist, IC50 221nM, 27x selective over GPR35/CB1/CB2, may aid Parkinson's symptoms.</p>

<p>RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.</p>

<p>JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.</p>

<p>β-Caryophyllene ((-)-(E)-Caryophyllene) acts as an CB2 receptor agonist.</p>

<p>Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and</p>

Polyphenol

Polyphenol

Quinone

Carboxylic acid with phenol function

Carboxylic acid with phenol function

Aromatic ether

Halogen derivative of polyphenol

Carboxylic acid with phenol function

Oxygen-heterocyclic compound

Carboxylic acid with phenol function

Polyphenol

<p>CB1/2 agonist 3 is a competitive and potent CB1/CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.</p>

<p>Applications (-)-Isoperitenone, is a derivative of (-)-Cannabidiol (C175300), a major, non psychotropic constituent of cannabis.<br>References Hanus, L. et al.: Organic &amp; Biomolecular Chemistry, Vol.3, Issue 6 (2005);<br></p>

<p>S-Methoprene (ZR2458), a juvenile hormone analog, acts as an insecticide influencing redox activity and male sex differentiation.</p>

<p>rel-(1R,2S)-8-Bromo-1-(3-bromo-4-hydroxy-5-methoxyphenyl)-1,2-dihydro-7-hydroxy-N2,N3-bis[2-(4-hydroxyphenyl)ethyl]-6-methoxy-2,3-naphthalenedicarboxamide is a synthetic chemical compound, which is derived through targeted organic synthesis and structural optimization efforts. Its source lies in advanced laboratory methodologies designed to enhance specific pharmacological properties. The mode of action is expected to involve selective interaction with particular molecular targets, potentially modulating distinct pathways related to cellular function or signaling processes.</p>

<p>A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).</p>

<p>1,2,3,9-Tetrahydro-4H-carbazol-4-one is a cyclic ketone compound, which can be synthesized through various organic reactions involving appropriate precursors. It is often derived from indole-based substrates through catalytic hydrogenation, allowing the formation of its stable tetrahydro structure with a retained core carbazole skeleton.</p>

<p>Positive allosteric modulator (PAM) of cannabinoid receptors CB2. The C2 modulator is the first synthetic PAM of CB2 receptors with antinociceptive properties, which were observed in a mouse model of neuropathic pain.</p>

<p>Cannabinoid type 1 (CB1) receptor agonist. Anti-depressant activity demonstrated in vivo alone, as well as enhancing the effect of fluoxetine. In the brain, ACEA activates CB1 receptors expressed in the mitochondria of neuronal cells to elicit neuroprotective effects. This is mediated by inducing glycogen synthase kinase-3β (GSK-3β) phosphorylation and inhibiting the opening of mitochondrial permeability transition pore (MPTP).<br>Sold by weight of solid</p>

<p>Anandamide is an endogenous cannabinoid, which is a bioactive lipid mediator primarily found in the brain and peripheral organs. It is synthesized from membrane phospholipid precursors through enzymatic pathways, primarily involving the enzyme N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD). Anandamide acts as a ligand for cannabinoid receptors, mainly the CB1 receptor located in the central nervous system, and the CB2 receptor found in peripheral tissues.</p>

<p>A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).</p>

<p>Cannabichromenic acid is a non-psychoactive phytocannabinoid and a precursor of cannabichromene1 which toxicological and pharmacological properties are unknown. Due to its structural similarity to cannabichromene, it is thought to reportedly exert anti-analgesic and anti-inflammatory activity.</p>

<p>A selective cannabinoid receptor type 2 (CB2) agonist. Commonly, CB2 agonists induce receptor internalization, which results in desensitization and tachyphylaxis. However, APD 371 mediates efficient recycling of internalized receptors back to the plasma membrane and thus sustains analgesic effects, upon subchronic treatment, in an osteoarthritis pain model in vivo.</p>

<p>Cannabigerovarinic acid is a phytocannabinoid and the precursor to tetrahydrocannabivarinic acid, cannabidivarinic acid, and cannabichromevarinic acid1. No in vitro or in vivo pharmacological and toxicological studies have been conducted on cannabigerovarinic acid.</p>

<p>Applications 5-(4-Hydroxypentyl)-1,3-benzenediol is an intermediate used in the synthesis of 4''-Hydroxycannabidiol (H824830), which is a metabolite of Canabidiol (C175300), a major constituents in marijuana. 4''-Hydroxycannabidiol be used to investigate canabidiol metabolism and human liver microsomes that metabolize Canabidiol into 6α-Hydroxycannabidiol.<br>References Jiang, R., et al.: Life Sci. 89, 165 (2011); Lander, N., et al.: Science 169, 611 (1970)<br></p>

Carboxylic acid with phenol function

<p>Dehydroabiethylamine (NSC-2955) boosts liver CYP2B, blocks PDKs &amp; cholesterol transport, and has anti-tumor effects.</p>

<p>Stability Light Sensitive<br>Applications (Z)-1-(3,5-Bis(benzyloxy)phenyl)pent-1-en-3-one is a reagent in the synthesis of 3''-Hydroxycannabidiol (H824825) which is a major constituents in marijuana. 3''-Hydroxycannabidiol be used to investigate canabidiol metabolism and human liver microsomes that metabolize Canabidiol into 6α-Hydroxycannabidiol.<br>References Jiang, R., et al.: Life Sci. 89, 165 (2011); Lander, N., et al.: Science 169, 611 (1970)<br></p>

<p>Applications Ethyl 2-oxopentanoate is used as a reagent to synthesize selective CB1 cannabinoid receptor antagonists. Ethyl 2-oxopentanoate is also used to synthesize derivatives of iminodiacid, an inhibitor of angiotensin converting enzyme.<br>References Lange, J., et al.: J. Med. Chem., 48, 1823 (2005); Vincent, M., et al.: Tetrahedron Lett., 23, 1677 (2982)<br></p>

<p>Stability Light Sensitive<br>Applications Cannabigerorcinic Acid is a compound that takes part in the biosynthesis of daurichromenic acid synthase which is active in anti-HIV biosynthesis.<br>References Iijima, M. et al.: Plant Phys., 174, 2213 (2017);<br></p>

<p>Applications 1-Methyl-4-(1-methylethenyl)-2-cyclohexen-1-ol is an acetal reagent used in the synthesis of desoxy cannabidiols and THC (T293202) related psychoactive compounds. It is formed from (+)-Limonene using a photosynthesized O2 transfer.<br>References Wilkinson, S. et al.: Tetrahedron Lett., 54, 52 (2013);<br></p>

<p>Applications 2-[(9Z)-9-Octadecenyloxy]-1,3-propanediol, which is an endogenous cannabinoid receptor ligand.<br>References Suhara, Y. et al.: Chem. Pharm. Bull., 48, 903 (2000);<br></p>

<p>2-Arachidonyl glycerol is an endogenous cannabinoid receptor agonist, which is derived from arachidonic acid present in cellular membranes. It functions as a signaling lipid and plays a critical role in the endocannabinoid system, which is a complex network of receptors and ligands involved in maintaining physiological homeostasis.</p>

<p>COR167 is a CB2 agonist with immunomodulatory effects, protective brain properties, and antinociception.</p>

<p>AM6538: long-acting, high-affinity CB antagonist similar to rimonabant, useful for studying cannabinoid agonists.</p>

<p>Arvanil (N-Vanillylarachidonamide) is a synthetic capsaicin-amphetamine hybrid that acts as a ligand for VR1 and CB1, offering neuroprotective effects.</p>

<p>CB2 agonist with Ki of 12.8 nM; EC50 of 38.67 nM. Negligible CB1 affinity, no GPR55 activity. Anti-inflammatory, neuroprotective, crosses BBB.</p>

<p>Compound 26, a GPR55 agonist, exhibits potent activity with EC50 values of 0.239 nM for hGPR55 and 1.76 nM for rGPR55.</p>

<p>NIDA 41020 is a CB1 receptor antagonist.</p>

<p>LH-21, a strong CB1 receptor antagonist, curbs eating and lessens weight gain in obese rats.</p>

<p>CID1792197 is a selective agonist of GPR55.</p>

<p>CB1R modulator 1 (compound 11), a potent CB1R inhibitor, decreases activity of orthosteric ligands.</p>

<p>PGN36 (Compound 18) is a potent CB2 receptor antagonist with a high affinity (Ki=0.09 μM).</p>