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Volumn 18, Issue 6, 2008, Pages 2006-2012

Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profiles

Author keywords

receptors; Opioid; Solid phase synthesis

Indexed keywords

3,4 DIMETHYL 4 (3 HYDROXYPHENYL)PIPERIDINE; ALVIMOPAN; LOPERAMIDE; MORPHINE; MU OPIATE RECEPTOR ANTAGONIST; NALOXONE; OPIATE RECEPTOR; PIPERIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 40749139396     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.01.106     Document Type: Article
Times cited : (5)

References (17)
  • 8
    • 0038248848 scopus 로고    scopus 로고
    • For a full description of the biological methods, see: Schlechtingen, G.; DeHaven, R. N.; Daubert, J. D.; Cassel, J. A.; Chung, N. N.; Schiller, P. W.; Taulane, J. P.; Goodman, M. sequence. Structure-activity relationships of dynorphin A analogs modified in the address J. Med. Chem. 2003, 46, 2104.
    • For a full description of the biological methods, see: Schlechtingen, G.; DeHaven, R. N.; Daubert, J. D.; Cassel, J. A.; Chung, N. N.; Schiller, P. W.; Taulane, J. P.; Goodman, M. sequence. Structure-activity relationships of dynorphin A analogs modified in the address J. Med. Chem. 2003, 46, 2104.
  • 15
    • 40749099598 scopus 로고    scopus 로고
    • 35S]GTPγS) binding to membranes containing δ opioid receptors.
    • 35S]GTPγS) binding to membranes containing δ opioid receptors.
  • 16
    • 40749126968 scopus 로고    scopus 로고
    • note
    • In vivo test methods: (a) Gastrointestinal Transit (GIT) assay: Male Swiss-Webster mice (20-25 g) were fasted overnight prior to the experiment. Mice were treated with vehicle (10% DMSO:20% cremophor EL:70% saline), or test compound (administered using the subcutaneous route). Twenty-five minutes after administration of vehicle or tested compound, the mice were treated with morphine (3 mg/kg s.c.), and 10 min later received 0.3 mL of a charcoal meal consisting of charcoal:flour:water (1:2:8, w/w/v). Gastrointestinal transit (GIT) was measured 25 min after the administration of the charcoal meal. GIT was determined by removing the entire length of the small intestine and measuring how far the leading edge of the charcoal meal traveled in the small intestine; % GIT was determined by the following formula: % GIT = [distance to charcoal leading edge (cm)/length of small intestine (cm)] × 100. (b) Assessment of physical dependence: male Swiss-Webster mice (30-35 g) were implanted with a placebo or a 75 mg morphine base pellet (Murty Pharmaceuticals, Inc., Lexington, KY). Three days after the pellet implantation, mice were treated with vehicle (10% DMSO:20% Cremophor EL:70% Saline) or test compound (administered using the subcutaneous route at the dose of 10 mg/kg). Immediately after the treatment, the mice were placed in individual plastic observation cylinders (26 cm high × 22 cm diameter) and the number of jumps and other abstinence behaviors were recorded for a 10 min period. One hour after the treatment, the incidence of diarrhea was assessed as absent or present for each mouse and a post treatment body weight was obtained.
  • 17
    • 40749140121 scopus 로고    scopus 로고
    • Le Bourdonnec, B.; Dolle, R. E. U.S. Patent 254218, 2004.
    • Le Bourdonnec, B.; Dolle, R. E. U.S. Patent 254218, 2004.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.