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DREADD Activators Small Molecules and Peptides

DREADD Mechanism of Action

The first DREADDs to be developed were derived from human muscarinic acetylcholine receptors (mAChRs) and termed hM1-5. These receptors have mutations in their orthosteric binding site, abolishing their affinity for the endogenous ligand ACh, while rendering them responsive to small molecule DREADD ligands, such as Clozapine-N-oxide (CNO, Cat. No. 4936) or Deschloroclozapine (DCZ, Cat. No. 7193).

The effect of ligand binding depends on the G protein-coupling of the ...

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Clozapine N-oxide (CNO)

Catalog #: 4936
(8)
Citations (530)
Product Documents

Activator of hM3Dq and hM4Di DREADDs

Alternate Names: CNO
Chemical Name: 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
Activator of hM3Dq and hM4Di DREADDs

Clozapine N-oxide dihydrochloride

Catalog #: 6329
(1)
Citations (100)
Product Documents

Activator of hM3Dq and hM4Di DREADDs; water soluble version of Clozapine N-oxide (Cat. No. 4936)

Alternate Names: CNO (water-soluble)
Chemical Name: 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
Purity: ≥99%
Activator of hM3Dq and hM4Di DREADDs; water soluble version of Clozapine N-oxide (Cat. No. 4936)

Deschloroclozapine

Catalog #: 7193
Citations (23)
Product Documents

High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapid blood-brain barrier penetrant

Alternate Names: DCZ
Chemical Name: 11-(4-Methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapidly blood brain barrier penetrant

DREADD agonist 21 dihydrochloride

Catalog #: 6422
Citations (17)
Product Documents

Potent hM3Dq and hM4Di DREADD agonist; water soluble version of DREADD agonist 21 (Cat. No. 5548)

Alternate Names: Compound 21 (water-soluble)
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
Purity: ≥98%
Potent hM3Dq and hM4Di DREADD agonist; water soluble version of DREADD agonist 21 (Cat. No. 5548)

Salvinorin B

Catalog #: 5611
(1)
Citations (12)
Product Documents

Activator of κ-opioid DREADD (KORD)

Chemical Name: (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(3-Furanyl)dodecahydro-9-hydroxy-6a,10b-dimethyl-4,10-dioxo-2H-naphtho[2,1-c]pyran-7-carboxylic acid methyl ester
Purity: ≥98%
Activator of κ-opioid DREADD (KORD)

JHU 37160

Catalog #: 7198
Citations (2)
Product Documents

High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant

Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant

DREADD agonist 21

Catalog #: 5548
(1)
Citations (22)
Product Documents

Potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant

Alternate Names: Compound 21,C21
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
Potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant

Olanzapine

Catalog #: 4349
Citations (19)
Product Documents

5-HT2A antagonist; also D2 antagonist; atypical antipsychotic

Chemical Name: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine
Purity: ≥98%
5-HT2A antagonist; also D2 antagonist; atypical antipsychotic

Perlapine

Catalog #: 5549
Citations (4)
Product Documents

Potent hM3Dq and hM4Di DREADD agonist in vitro

Chemical Name: 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
Purity: ≥99%
Potent hM3Dq and hM4Di DREADD agonist in vitro

JHU 37152

Catalog #: 7197
Product Documents

High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant

Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant

MOMBA

Catalog #: 7926
Citations (1)
Product Documents

Selective orthostatic agonist of hFFA2-DREADDs

Chemical Name: 4-Methoxy-3-methylbenzoic acid
Purity: ≥98%
Selective orthostatic agonist of hFFA2-DREADDs
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