Etoxadrol binding does not affect the binding affinity of other sites on the NMDA receptor, as found by binding studies showing the displacement of radiolabeledTCP 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]
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 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 produces a wide variety of dreams, ranging from pleasant to frightening or aversive.[11] Approximately half of patients given etoxadrol report pleasant dreams, 25% report unpleasant dreams, and the remaining 25% experience no dreams at all. Such dreams were frequently described as “floating,” “puffy” or “out of this world." Dreams and 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]
^ abThurkauf A, Zenk PC, Balster RL, May EL, George C, Carroll FI, et al. (December 1988). "Synthesis, absolute configuration, and molecular modeling study of etoxadrol, a potent phencyclidine-like agonist". Journal of Medicinal Chemistry. 31 (12): 2257–63. doi:10.1021/jm00120a004. PMID2903930.
^Thurkauf A, Mattson MV, Richardson S, Mirsadeghi S, Ornstein PL, Harrison EA, et al. (April 1992). "Analogues of the dioxolanes dexoxadrol and etoxadrol as potential phencyclidine-like agents. Synthesis and structure-activity relationships". Journal of Medicinal Chemistry. 35 (8): 1323–9. doi:10.1021/jm00086a001. PMID1349351.
^ abSax M, Wünsch B (2006). "Relationships between the structure of dexoxadrol and etoxadrol analogues and their NMDA receptor affinity". Current Topics in Medicinal Chemistry. 6 (7): 723–32. doi:10.2174/156802606776894483. PMID16719812.
^Aepkers M, Wünsch B (December 2005). "Structure-affinity relationship studies of non-competitive NMDA receptor antagonists derived from dexoxadrol and etoxadrol". Bioorganic & Medicinal Chemistry. 13 (24): 6836–49. doi:10.1016/j.bmc.2005.07.030. PMID16169732.
^ abcdefFrederickson EL, Longnecker DE, Allen GW (May–Jun 1976). "Clinical investigation of a new intravenous anesthetic--etoxadrol hydrochloride (CL-1848; U-37862A)". Anesthesia and Analgesia. 55 (3): 335–9. doi:10.1213/00000539-197605000-00010. PMID5921. S2CID45801472.
^ abcBrady KT, Woolverton WL, Balster RL (January 1982). "Discriminative stimulus and reinforcing properties of etoxadrol and dexoxadrol in monkeys". The Journal of Pharmacology and Experimental Therapeutics. 220 (1): 56–62. PMID6118431.
^ abThurkauf A, Mattson MV, Huguenin PN, Rice KC, Jacobson AE (October 1988). "Etoxadrol-meta-isothiocyanate: a potent, enantioselective, electrophilic affinity ligand for the phencyclidine-binding site". FEBS Letters. 238 (2): 369–74. doi:10.1016/0014-5793(88)80514-3. PMID2901991. S2CID22308090.
^ abcTraber DL, Priano LL, Wilson RD (November 1970). "Effects of CL 1848C, a new dissociative anesthetic, on the canine cardiovascular and respiratory systems". The Journal of Pharmacology and Experimental Therapeutics. 175 (2): 395–403. PMID5481707.