Etoxadrol

Source: Wikipedia, the free encyclopedia.
Etoxadrol
Clinical data
ATC code
  • none
Legal status
Legal status
  • In general: legal
Identifiers
  • (2S)-2-[(2S,4S)-2-ethyl-2-phenyl-1,3-dioxolan-4-yl]piperidine
JSmol)
  • CC[C@]1(C2=CC=CC=C2)OC[C@H]([C@H]3NCCCC3)O1
  • InChI=1S/C16H23NO2/c1-2-16(13-8-4-3-5-9-13)18-12-15(19-16)14-10-6-7-11-17-14/h3-5,8-9,14-15,17H,2,6-7,10-12H2,1H3/t14-,15+,16-/m0/s1 checkY
  • Key:INOYCBNLWYEPSB-XHSDSOJGSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Etoxadrol (CL-1848C) is a

hallucinations.[3][4][5]

Chemical structure

Phencyclidine (PCP), ketamine, etoxadrol and dexoxadrol all contain phenyl and amino groups, which bind to the PCP site on the NMDA receptor. Tenocyclidine contains a thiophene ring instead, which is bioisosteric with a phenyl ring.

dissociative hallucinogens (meaning that they interfere with normal sensory signals, replacing them with hallucinations of any sensory modality) with anesthetic and analgesic
properties.

Pharmacodynamics

Etoxadrol is a

cations from entering or exiting the channel. This mechanism of action also applies to PCP, TCP, ketamine and dexoxadrol
.

Etoxadrol binding does not affect the binding affinity of other sites on the NMDA receptor, as found by binding studies showing the displacement of radiolabeled TCP by etoxadrol (TCP binding in the absence of etoxadrol: Ki = 19.2 x 10−9 M, Bmax = 1.36 pmol/mg protein; TCP binding in the presence of etoxadrol: Ki = 21.7 x 10−9 M, Bmax = .66 pmol/mg protein).[9]

Despite its

mu opioid receptors.[9] However, etoxadrol may act in the dopamine reward pathway, explaining its reinforcing properties.[6]

Pharmacokinetics

Etoxadrol goes into effect 90 seconds after

intravenous (IV) administration, and its anesthetic effects typically last for half an hour to an hour.[5][10] Since etoxadrol is administered intravenously, the bioavailable dose is always the same as the administered dose. Etoxadrol's analgesic effects can last for up to 2 hours or more after patients have regained consciousness.[11]

Etoxadrol is

cardiovascular systems.[10]

Treatment

Etoxadrol was intended as an anesthetic for patients requiring particularly long periods of anesthesia for surgery. As an anesthetic, etoxadrol is more potent than ketamine, but less potent than PCP.[11]

Etoxadrol is also a potent analgesic. Patients given etoxadrol often reported that they were aware of experiencing pain upon waking from anesthesia, but it did not bother them.[5] Post-operative analgesics are rarely required after patients undergoing surgery are administered etoxadrol.

Etoxadrol (along with

seizures.[12]

Side effects

Like

Monkeys given extremely high (> 20 mg/kg) doses of etoxadrol died of apparent respiratory failure
.

Etoxadrol produces a wide variety of

hallucinations may persist for as long as 18 to 24 hours. In rare cases, etoxadrol can induce periods of psychotic activity during this recovery period.[5]

In the brain, etoxadrol slows down the synthesis of serotonin to 50-60% of control rates and speeds up the rate of dopamine synthesis by up to 200% of the normal rate 4–6 hours after intravenous administration.[5]

Like a number of other

Monkeys will self-administer etoxadrol, dexoxadrol or PCP in a lever-pressing paradigm.[6]

References

  1. ^
    PMID 2903930
    .
  2. PMID 1349351
    .
  3. ^
    PMID 16719812
    .
  4. PMID 16169732
    .
  5. ^
    S2CID 45801472
    .
  6. ^
    PMID 6118431
    .
  7. S2CID 17738916
    .
  8. ISBN 978-0781760034
    .
  9. ^
    S2CID 22308090
    .
  10. ^
    PMID 5481707
    .
  11. ^
    S2CID 33036876
    .
  12. PMID 4085541
    .
  13. S2CID 29976263
    .
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