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Research tools

AM630Also known as 6-iodopravadoline

Selective inverse agonist of the CB2 receptor, a laboratory tool.

FranceNarcotic: generic clauseInternationalUnscheduled
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.

C₂₃H₂₅IN₂O₃

CAS 164178-33-0

Family
ECS pharmacological toolAntagonist or inverse agonist
Molar mass
504.40 g/mol

Updated on

In plain terms

AM630 is a laboratory reagent, not a consumer substance. Researchers use it to block the CB2 receptor and check that an observed effect really goes through it. Its structure nevertheless brings it, in France, under a general definition aimed at synthetic cannabinoids.

Receptors and activity

Target network

CB2Inverse agonistKi = 31.2 nM · humanmembranes of CHO cells expressing human CB2, [3H]CP 55,940 displacement
  • Activates
  • Blocks or inhibits

The lower the cited value, the closer the target sits to AM630: 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 AM630.

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. CB2Inverse agonistKi = 31.2 nM · human58 out of 100

    Ross et al., Br J Pharmacol 1999 (new tab) · membranes of CHO cells expressing human CB2, [3H]CP 55,940 displacement

  2. CB1Partial agonistno 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

AM630 (6-iodopravadoline) is a synthetic aminoalkylindole, derived from pravadoline, used in the laboratory to study CB2-mediated responses. Presented in 1995 as a competitive antagonist of cannabinoid receptors in the mouse vas deferens (Pertwee et al. 1995), it was characterised in 1999 on recombinant human receptors: Ki of 31.2 nM at CB2 and a CB2/CB1 affinity ratio of 165; inverse agonist at CB2 (5.2-fold enhancement of forskolin-stimulated cAMP at 1 µM) and weak partial agonist at CB1 (Ross et al. 1999). An inverse agonist lowers the receptor's constitutive activity instead of merely blocking agonist access, which can produce an effect of its own in the absence of any ligand. In Idris et al. (2008), osteoclasts from CB2 knockout mice were resistant to the inhibitory effect of AM630 seen in vitro on wild-type osteoclasts, which ties that effect to CB2.

Key sources.

History

Source
A synthetic molecule of the aminoalkylindole class, absent from cannabis and from any living organism. A research reagent used in cannabinoid-receptor pharmacology.

Origin

Research tool

No biosynthetic pathway: a synthetic molecule, the 6-iodo analogue of pravadoline.

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Antagonist or inverse agonist

Verification

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

Wikipedia (English)

AM-630 (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. Ross RA, Brockie HC, Stevenson LA et al., Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630, British Journal of Pharmacology 1999 (new tab)PMID 10188977
  2. Pertwee RG, Griffin G, Fernando S et al., AM630, a competitive cannabinoid receptor antagonist, Life Sciences 1995 (new tab)PMID 7776818
  3. Idris AI et al., Regulation of bone mass, osteoclast function and ovariectomy-induced bone loss by the type 2 cannabinoid receptor, Endocrinology 2008, example of the use of AM630 as a tool (new tab)PMID 18635663
  4. ANSM, consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV, heading « Indol-3-yl methanone » (new tab)
  5. PubChem, Compound Summary CID 4302963, AM-630 (new tab)

Identifiers

Names

Common name
AM630 (6-iodopravadoline)
IUPAC name
[6-iodo-2-methyl-1-(2-morpholin-4-ylethyl)indol-3-yl]-(4-methoxyphenyl)methanone
Other names
AM 630 · 6-iodopravadoline · iodopravadoline

Identifiers

Formula
C₂₃H₂₅IN₂O₃
CAS
164178-33-0
PubChem CID
4302963(new tab)
ChEBI
93112(new tab)
InChIKey
JHOTYHDSLIUKCJ-UHFFFAOYSA-N
SMILES
CC1=C(C2=C(N1CCN3CCOCC3)C=C(C=C2)I)C(=O)C4=CC=C(C=C4)OC

Machine-readable entry (JSON)

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