GP1a is a potent agonist of cannabinoid receptor 2 (CB2). Gp1a is beneficial to skin wound healing. GP1a inhibits inflammation and fibrogenesis while promoting re-epithelialization.

GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.

N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM.

Pravadoline is a cannabimimetic aminoalkylindole agonist of the cannabinoid receptors and an inhibitor of Cox-1 and Cox-2, demonstrating powerful analgesic effects through the combination of these actions.

CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.

Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual CB1 receptor/iNOS inhibitor.Zevaquenabant ((S)-MRI-1867) (3 mg/kg, p.o.) ameliorated obesity-induced kidney morphological and functional changes via decreasing kidney inflammation, fibrosis, oxidative stress, and renal injury.The hybrid CB1R/iNOS inhibitor Zevaquenabant ((S)-MRI-1867) has greater antifibrotic efficacy than inhibition of CB1R alone.(S)-MRI-1867 reduced hepatic steatosis and the rate of hepatic VLDL secretion, upregulated hepatic LDLR expression, and reduced the circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9) in diet-induced obesity (DIO mice).

RTICBM-74 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with IC50 of 23 nM in Ca2+ assays.RTICBM-74 displays excellent half-life and low clearance against rat liver microsomes and hepatocytes, and excellent brain penetrance in rats.RTICBM-74 specifically reduces alcohol intake across a range of doses in male or female Wistar or Long-Evans rats, reduces alcohol intake and does not affect locomotion or sucrose self-administration.

RTICBM-229 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with IC50 of 169 nM in Ca2+ assay, 40 nM in GTPγS assay.

CB65 is a potent and high affinity CB2 selective agonist with a Ki value of 3.3 nM. CB65 exhibits a Ki of >1000 nM for CB1 receptor.

Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin.

CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively. IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R) Target: CB1R in vivo: CB1-IN-1 is a novel peripherally restricted cannabinoid 1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. CB1-IN-1 has great potential to ameliorate this related metabolic syndrome.

Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.

S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.

(±)-SLV 319 is a potent and selective CB1 receptor antagonist (Ki = 7.8 nM). Exhibits 1000-fold selectivity for CB1 over CB2 receptors.

5,3-AB-CHMFUPPYCA is an analytical reference standard that is structurally classified as a synthetic cannabinoid.

AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively.

BML-190 is an indomethacin morpholinylamide which functions as a selective inverse agonist of the human cannabinoid CB2 receptor.

Vicasinabin is the potent agonist of cannabinoid receptor 2 (CB2). Vicasinabin has the potential for the research of human diseases including chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and other related diseases (extracted from patent US20130116236A1).

LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).

CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).

RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).

CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.

RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).

AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist. AZD1940 shows a robust analgesia action.

2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.

Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.

Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.

Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models.