SR-16435

SR-16435
Identifiers
	IUPAC name 1-[1-(9-bicyclo[3.3.1]nonanyl)piperidin-4-yl]-3H-indol-2-one;
CAS Number	857262-16-9;
PubChem CID	11461888;
Chemical and physical data
Formula	C22H30N2O
Molar mass	338.495 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CC2CCCC(C1)C2N3CCC(CC3)N4C(=O)CC5=CC=CC=C54;
	InChI InChI=1S/C22H30N2O/c25-21-15-18-5-1-2-10-20(18)24(21)19-11-13-23(14-12-19)22-16-6-3-7-17(22)9-4-8-16/h1-2,5,10,16-17,19,22H,3-4,6-9,11-15H2; Key:XVFXJQGBDPFCRF-UHFFFAOYSA-N;

SR-16435 is a drug which acts as a potent partial agonist at both the μ-opioid receptor and nociceptin receptor. In animal studies it was found to be a potent analgesic, with results suggestive of reduced development of tolerance and increased activity against neuropathic pain compared to classic μ-selective agonists.^[1]^[2]^[3]

References

^ Khroyan TV, Zaveri NT, Polgar WE, Orduna J, Olsen C, Jiang F, Toll L (February 2007). "SR 16435 [1-(1-(bicyclo[3.3.1]nonan-9-yl)piperidin-4-yl)indolin-2-one], a novel mixed nociceptin/orphanin FQ/mu-opioid receptor partial agonist: analgesic and rewarding properties in mice". The Journal of Pharmacology and Experimental Therapeutics. 320 (2): 934–43. doi:10.1124/jpet.106.111997. PMID 17132815. S2CID 2920534.
^ Spagnolo B, Calo G, Polgar WE, Jiang F, Olsen CM, Berzetei-Gurske I, et al. (February 2008). "Activities of mixed NOP and mu-opioid receptor ligands". British Journal of Pharmacology. 153 (3): 609–19. doi:10.1038/sj.bjp.0707598. PMC 2241792. PMID 18059322.
^ Sukhtankar DD, Zaveri NT, Husbands SM, Ko MC (July 2013). "Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain". The Journal of Pharmacology and Experimental Therapeutics. 346 (1): 11–22. doi:10.1124/jpet.113.203984. PMC 3684842. PMID 23652222.

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[1] Khroyan TV, Zaveri NT, Polgar WE, Orduna J, Olsen C, Jiang F, Toll L (February 2007). "SR 16435 [1-(1-(bicyclo[3.3.1]nonan-9-yl)piperidin-4-yl)indolin-2-one], a novel mixed nociceptin/orphanin FQ/mu-opioid receptor partial agonist: analgesic and rewarding properties in mice". The Journal of Pharmacology and Experimental Therapeutics. 320 (2): 934–43. doi:10.1124/jpet.106.111997. PMID 17132815. S2CID 2920534.

[2] Spagnolo B, Calo G, Polgar WE, Jiang F, Olsen CM, Berzetei-Gurske I, et al. (February 2008). "Activities of mixed NOP and mu-opioid receptor ligands". British Journal of Pharmacology. 153 (3): 609–19. doi:10.1038/sj.bjp.0707598. PMC 2241792. PMID 18059322.

[3] Sukhtankar DD, Zaveri NT, Husbands SM, Ko MC (July 2013). "Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain". The Journal of Pharmacology and Experimental Therapeutics. 346 (1): 11–22. doi:10.1124/jpet.113.203984. PMC 3684842. PMID 23652222.

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See also

References