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Synthetic

APD371Olorinab (APD371)

A peripherally acting full CB2 agonist, trialled in digestive pain without demonstrated efficacy.

Unscheduled
Level of detail

Harm-reduction warning

No characterised human dose: animal / in vitro data only. Effect profile, safety margin and acute toxicity are not documented in human clinical practice. Extremely potent compound: severe effects, seizures and deaths reported in the literature.

C₁₈H₂₃N₅O₃

CAS 1268881-20-4

Family
Synthetic CB receptor agonistResearch ligand or medicine
Molar mass
357.40 g/mol

Updated on

In plain terms

Olorinab, also called APD371, is a laboratory molecule developed by a pharmaceutical company: it does not come from hemp and is in no product on sale. It targets only the CB2 receptor, found mainly outside the brain. It was studied for the digestive pain of Crohn's disease and then irritable bowel syndrome; in the controlled trial, it did not differ from placebo on the primary endpoint.

Receptors and activity

Target network

CB2AgonistEC50 = 6.2 nM · humanrecombinant CB2 in HEK293 cells; Emax 106%; 7.6 nM at rat CB2 (Emax 100%)
  • Activates

The lower the cited value, the closer the target sits to APD371: one ring per factor of 100. A target with no measured value stays on the edge.

Where these targets live

Where each target has been found in humans, according to the cited studies. The map shows the target, not an effect of APD371.

Brain, side view
Body, front view
Blood

CB2CB2 found in 5 regions of the body

  1. SpleendenseHighly abundant in the spleen1
  2. Immune cellspresentMainly B cells and natural killer cells1
  3. SkinpresentKeratinocytes, mast cells and nerve fibres2
  4. GutpresentImmune cells of the colonic mucosa3
  5. BonepresentPresent on osteoclasts4

Map sources

  1. Galiègue S et al. Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations. Eur J Biochem, 1995 (new tab)
  2. Ständer S et al. Distribution of cannabinoid receptor 1 (CB1) and 2 (CB2) on sensory nerve fibers and adnexal structures in human skin. J Dermatol Sci, 2005 (new tab)
  3. Wright K et al. Differential expression of cannabinoid receptors in the human colon: cannabinoids promote epithelial wound healing. Gastroenterology, 2005 (new tab)
  4. Rossi F et al. The endovanilloid/endocannabinoid system in human osteoclasts: possible involvement in bone formation and resorption. Bone, 2009 (new tab)

Cited values

  1. CB2AgonistEC50 = 6.2 nM · human70 out of 100

    Han et al., ACS Med Chem Lett 2017 (ChEMBL values from the document) (new tab) · recombinant CB2 in HEK293 cells; Emax 106%; 7.6 nM at rat CB2 (Emax 100%)

  2. CB1Agonistno measured value cited
Bar length follows the measured value (Ki, Kd, EC50 or IC50), on one scale shared by every entry, from 100 µM to 0.1 nM. A target with no cited value has no bar.

Pharmacology

Olorinab is a full and highly selective agonist of the cannabinoid CB2 receptor, designed to act in the periphery. In recombinant systems, its median effective concentration is 6.2 nM at human CB2 and 7.6 nM at rat CB2, with a maximal effect equal to or slightly above that of CP-55,940, whereas no activation of CB1 is measured below 10,000 nM, a functional selectivity of more than 1,000-fold (Han et al. 2017). The brain-to-plasma ratio measured in the rat, about 0.04, indicates low brain penetration. In rodents, the molecule reduced visceral hypersensitivity in models of colitis and chronic visceral hypersensitivity, with no effect in control animals, in a CB2-dependent way (Castro et al. 2022). In humans, an open-label randomised phase 2a study in fourteen patients with Crohn's disease showed a fall in abdominal pain scores, without a control group (Yacyshyn et al. 2021). The controlled phase 2b trial CAPTIVATE, run in 273 people with irritable bowel syndrome, did not meet its primary endpoint: the change in average abdominal pain score at twelve weeks did not differ from placebo for the three doses studied; only a prespecified subgroup analysis (high baseline pain) favoured the highest dose (Chang et al. 2023). Clinical efficacy is therefore not established, and no phase 3 trial was found in the sources consulted.

Key sources.

History

Source
An entirely synthetic molecule with no natural occurrence: it exists neither in cannabis, nor in any other plant, nor in the human body. It was designed in a pharmaceutical laboratory as a drug candidate targeting the CB2 receptor in the periphery, then evaluated in humans for abdominal pain in Crohn's disease and irritable bowel syndrome. It is present in no consumer product and is marketed nowhere.

Origin

Laboratory synthesis

No biosynthetic pathway: the molecule comes from no living organism. It is a heterocyclic carboxamide obtained by organic synthesis, combining a pyrazole fused to a cyclopropane-bridged carbocycle, a pyrazine N-oxide borne on the pyrazole nitrogen, and an amino alcohol derived from tert-leucine.

Classification

Family, origin and source verification

Family

Synthetic CB receptor agonist › Research ligand or medicine

Class

pyrazole-3-carboxamide

Verification

Classification, sources and binding values checked on 20 October 2026; text read against its sources and Wikipedia.

Wikipedia (English)

Olorinab (new tab)

Article paired by the molecule's structure (InChIKey), revision read on 19 October 2026. Read as a second opinion, never cited as a source.

References

  1. Han S et al., Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain, ACS Med Chem Lett 2017 (new tab)PMID 29259753
  2. Castro J et al., Olorinab (APD371), a peripherally acting, highly selective, full agonist of the cannabinoid receptor 2, reduces colitis-induced acute and chronic visceral hypersensitivity in rodents, Pain 2022 (new tab)PMID 33863856
  3. Yacyshyn BR et al., Safety, Pharmacokinetics, and Efficacy of Olorinab in a Phase 2a Study of Patients With Chronic Abdominal Pain Associated With Crohn's Disease, Crohn's & Colitis 360 (new tab)PMID 36777064
  4. Chang L et al., Efficacy and safety of olorinab for the treatment of abdominal pain in patients with irritable bowel syndrome, phase 2b CAPTIVATE trial, Neurogastroenterol Motil 2023 (new tab)PMID 36740814
  5. Camilleri M and Zheng T, Cannabinoids and the Gastrointestinal Tract, Clin Gastroenterol Hepatol 2023 (new tab)PMID 37678488

Identifiers

Names

Common name
Olorinab (APD371)
IUPAC name
(2S,4S)-N-[(2S)-1-hydroxy-3,3-dimethylbutan-2-yl]-9-(4-oxidopyrazin-4-ium-2-yl)-8,9-diazatricyclo[4.3.0.02,4]nona-1(6),7-diene-7-carboxamide
Other names
APD371 · APD-371 · Olorinab · olorinab

Identifiers

Formula
C₁₈H₂₃N₅O₃
CAS
1268881-20-4
PubChem CID
60164925(new tab)
InChIKey
ACSQLTBPYZSGBA-GMXVVIOVSA-N
SMILES
CC(C)(C)[C@@H](CO)NC(=O)C1=NN(C2=C1C[C@H]3[C@@H]2C3)C4=NC=C[N+](=C4)[O-]

Machine-readable entry (JSON)

LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.