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Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Bioorg Med Chem Lett. 2011 Apr 15; 21(8):2359-64.BM

Abstract

A novel series of decahydroquinoline CB2 agonists is described. Optimization of the amide substituent led to improvements in CB2/CB1 selectivity as well as physical properties. Two key compounds were examined in the rat CFA model of acute inflammatory pain. A moderately selective CB2 agonist was active in this model. A CB2 agonist lacking functional CB1 activity was inactive in this model despite high in vivo exposure both peripherally and centrally.

Authors+Show Affiliations

Department of Medicinal Chemistry, Merck Research Laboratories, West Point PA, United States. peter_manley@merck.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21420857

Citation

Manley, Peter J., et al. "Decahydroquinoline Amides as Highly Selective CB2 Agonists: Role of Selectivity On in Vivo Efficacy in a Rodent Model of Analgesia." Bioorganic & Medicinal Chemistry Letters, vol. 21, no. 8, 2011, pp. 2359-64.
Manley PJ, Zartman A, Paone DV, et al. Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia. Bioorg Med Chem Lett. 2011;21(8):2359-64.
Manley, P. J., Zartman, A., Paone, D. V., Burgey, C. S., Henze, D. A., Della Penna, K., Desai, R., Leitl, M. D., Lemaire, W., White, R. B., Yeh, S., Urban, M. O., Kane, S. A., Hartman, G. D., Bilodeau, M. T., & Trotter, B. W. (2011). Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia. Bioorganic & Medicinal Chemistry Letters, 21(8), 2359-64. https://doi.org/10.1016/j.bmcl.2011.02.078
Manley PJ, et al. Decahydroquinoline Amides as Highly Selective CB2 Agonists: Role of Selectivity On in Vivo Efficacy in a Rodent Model of Analgesia. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2359-64. PubMed PMID: 21420857.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia. AU - Manley,Peter J, AU - Zartman,Amy, AU - Paone,Daniel V, AU - Burgey,Christopher S, AU - Henze,Darrell A, AU - Della Penna,Kimberly, AU - Desai,Reshma, AU - Leitl,Michael D, AU - Lemaire,Wei, AU - White,Rebecca B, AU - Yeh,Suzie, AU - Urban,Mark O, AU - Kane,Stefanie A, AU - Hartman,George D, AU - Bilodeau,Mark T, AU - Trotter,B Wesley, Y1 - 2011/02/26/ PY - 2010/11/10/received PY - 2011/02/16/revised PY - 2011/02/22/accepted PY - 2011/3/23/entrez PY - 2011/3/23/pubmed PY - 2011/7/20/medline SP - 2359 EP - 64 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 21 IS - 8 N2 - A novel series of decahydroquinoline CB2 agonists is described. Optimization of the amide substituent led to improvements in CB2/CB1 selectivity as well as physical properties. Two key compounds were examined in the rat CFA model of acute inflammatory pain. A moderately selective CB2 agonist was active in this model. A CB2 agonist lacking functional CB1 activity was inactive in this model despite high in vivo exposure both peripherally and centrally. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/21420857/Decahydroquinoline_amides_as_highly_selective_CB2_agonists:_role_of_selectivity_on_in_vivo_efficacy_in_a_rodent_model_of_analgesia_ DB - PRIME DP - Unbound Medicine ER -