| 词条 | Cyclazocine |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 460109436 | IUPAC_name = 3-(Cyclopropylmethyl)-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-8-ol or 2-Cyclopropylmethyl-2'-hydroxy-5,9-dimethyl-6,7-benzomorphan | image = Cyclazocine structure.svg | width = 200 | tradename = | pregnancy_category = | legal_status = | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|changed|CAS}} | CAS_number = 3572-80-3 | ATC_prefix = none | ATC_suffix = | PubChem = 19143 | IUPHAR_ligand = 1604 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 18063 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = J5W1B1159C | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D03618 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 56585 | C=18 | H=25 | N=1 | O=1 | molecular_weight = 271.40 g/mol | smiles = Oc1ccc4c(c1)C2(C(C(N(CC2)CC3CC3)C4)C)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C18H25NO/c1-12-17-9-14-5-6-15(20)10-16(14)18(12,2)7-8-19(17)11-13-3-4-13/h5-6,10,12-13,17,20H,3-4,7-9,11H2,1-2H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = YQYVFVRQLZMJKJ-UHFFFAOYSA-N }}Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines.[1] It is a KOR agonist and MOR partial agonist, and also has high affinity for the DOR.[2] UseResearch into the use of cyclazocine for the treatment of bipolar patients with depression was undertaken by Fink and colleagues (1970). It showed that 8 out of 10 patients experienced moderate improvement. Research during the 1960s and 1970s into the possible use of cyclazocine for management of pain, and later for assisting treatment of narcotic addiction was severely hampered by the drug's psychotomimetic, dysphoric, and hallucinatory effects.[3] The dysphoric/anxiety inducing effects the drug correlate with increasing dosage and would likely reduce the risk of abuse in the same manner as other opioids which preferentially act on the KOR versus the DOR. and MOR, although the side-effect threshold is often lower than the lowest effective dose. See also
References1. ^{{ cite journal | author = Archer, S. | author2 = Glick, S. D. | author3 = Bidlack, J. M. | title = Cyclazocine Revisited | journal = Neurochemical Research | year = 1996 | volume = 21 | issue = 11 | pages = 1369–1373 | doi = 10.1007/BF02532378 | pmid = 8947927 | url = }} {{Analgesics}}{{Hallucinogens}}{{Opioid receptor modulators}}{{Sigma receptor modulators}}2. ^{{cite journal | vauthors = Bidlack JM, Cohen DJ, McLaughlin JP, Lou R, Ye Y, Wentland MP | title = 8-Carboxamidocyclazocine: a long-acting, novel benzomorphan | journal = J. Pharmacol. Exp. Ther. | volume = 302 | issue = 1 | pages = 374–80 |date=July 2002 | pmid = 12065740 | doi = 10.1124/jpet.302.1.374| url = }} 3. ^{{ cite journal | url = http://jama.ama-assn.org/content/202/3/191.full.pdf | author = Freedman, A. M. | author2 = Fink, M. | author3 = Sharoff, R. | author4 = Zaks, A. | title = Cyclazocine and Methadone in Narcotic Addiction | journal = The Journal of the American Medical Association | year = 1967 | volume = 202 | issue = 3 | pages = 191–194 | doi = 10.1001/jama.1967.03130160065011 | pmid = 6072354 }} 4 : Synthetic opioids|Phenols|Benzomorphans|Kappa agonists |
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