Water-soluble Compound 21 (DREADD agonist 21) can be used as an alternative to clozapine N-oxide (water soluble), or to supplement CNO studies. Compound 21 has a similar in vivo potency to CNO, but is less likely to metabolize to clozapine.
Bristol, UK (PRWEB UK) 11 August 2017
GPCRs can be modified so that they only respond to a specific biologically inert chemical (a designer drug). These modified GPCRs are called Designer Receptors Exclusively Activated by Designer Drugs or “DREADDs”. Cells expressing DREADDs respond robustly to low concentrations of the designer molecule, whereas cells that do not express DREADD are unresponsive to the designer drug.
A recent publication in Science has reported that the traditionally used DREADD agonist clozapine N-oxide may have more off-target effects in vivo, than previously thought. Therefore pharmacological tools that offer additional ways to investigate DREADDs are of great use to researchers in this field.
Water-soluble Compound 21 (DREADD agonist 21) can be used as an alternative to clozapine N-oxide (water soluble), or to supplement CNO studies. Compound 21 has a similar in vivo potency to CNO, but is less likely to metabolize to clozapine. It offers another option for researchers studying DREADDs. And of course, in keeping with our ethos – it is offered at a very low price.
Steve Roome PhD, Managing Director and Founder, Hello Bio
Water soluble Compound 21 (DREADD agonist 21) joins a range of affordable and high quality tools for GPCR and DREADDs research, including DREADD ligands clozapine N-oxide and salvinorin B, and the novel GRK2/3 inhibitor Cmpd101, that can be used to study GPCR desensitisation.
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(0)117 3180 505
For full details of the Science publication, see: Gomez et al., Science 357, 503–507 (2017) Chemogenetics revealed: DREADD occupancy and activation via converted clozapine
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