New non-CNO actuators for DREADDs

Something we've been working on for a while now on-line and were funded by the BRAIN Initiative.
These non-CNO compounds are available from Jian Jin.

Several of these will have significant advantages over CNO for moving the technology forward to primates including the approved medication perlapine (Hypnodin(R)) which shows >1000-fold selectivity for hM3Dq.


Comments

  1. UnknownOctober 15, 2015 at 8:12 PM

    I am new in the field of DREADD. First, I find our blog very informative thank you very much. Moreover, I have a question about the non-CNO activator for DREADD. In this publication, the different compound were tested on hM3Dq : do you test one or all of these compound on hM4Di? or do you stipulate that like for CNO the compound that work on hM3Dq will also activate the hM4Di thus inhibit neuronal activity?
    Thanks in avdance for your answer!

    ReplyDelete
  2. zendudestOctober 16, 2015 at 6:23 AM

    They work just fine at hM4D

    ReplyDelete
  3. DREADDheadJuly 21, 2016 at 1:58 PM

    Have you or anyone looked at binding efficacy of perlapine at hM3/4D compared to 5HT, DA, NE, or other GPCRs yet?

    ReplyDelete
    Replies
    1. zendudestJuly 21, 2016 at 6:26 PM

      I believe if you look at the paper you will find that data

      Delete
    2. DREADDheadJuly 21, 2016 at 9:56 PM

      unless i am missing something, the paper does not compare perlapine to anything besides CNO or ACh (fig 3), and perlapine is not included in Table 2, where compounds are screened for activity at various other receptors.

      Delete
    3. zendudestJuly 25, 2016 at 7:14 AM

      Perlapine has been screened before and the data are in KiDB

      http://kidbdev.med.unc.edu/databases/pdsp.php

      Delete

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