University of Hertfordshire

BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys

Research output: Contribution to journalConference article

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BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys. / Ding, Huiping ; Czoty, Paul ; Cami-Kobeci, Gerta; Sukhtankar, Devki ; Nader, Michael ; Husbands, Stephen ; Ko, Mei-Chuan .

In: FASEB Journal, Vol. 29, No. 1, 616.2, 01.04.2015.

Research output: Contribution to journalConference article

Harvard

Ding, H, Czoty, P, Cami-Kobeci, G, Sukhtankar, D, Nader, M, Husbands, S & Ko, M-C 2015, 'BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys', FASEB Journal, vol. 29, no. 1, 616.2. https://doi.org/10.1096/fasebj.29.1_supplement.616.2

APA

Ding, H., Czoty, P., Cami-Kobeci, G., Sukhtankar, D., Nader, M., Husbands, S., & Ko, M-C. (2015). BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys. FASEB Journal, 29(1), [616.2]. https://doi.org/10.1096/fasebj.29.1_supplement.616.2

Vancouver

Ding H, Czoty P, Cami-Kobeci G, Sukhtankar D, Nader M, Husbands S et al. BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys. FASEB Journal. 2015 Apr 1;29(1). 616.2. https://doi.org/10.1096/fasebj.29.1_supplement.616.2

Author

Ding, Huiping ; Czoty, Paul ; Cami-Kobeci, Gerta ; Sukhtankar, Devki ; Nader, Michael ; Husbands, Stephen ; Ko, Mei-Chuan . / BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys. In: FASEB Journal. 2015 ; Vol. 29, No. 1.

Bibtex

@article{c9ef4390359a4a1985e215eab34c0574,
title = "BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys",
abstract = "BU08028, a novel buprenorphine analog, displays similar receptor binding profile like buprenorphine but with improved binding affinity and efficacy on nociceptin/orphanin FQ peptide (NOP) receptors. The aim of this study was to characterize the pharmacological profile of BU08028 as an analgesic in rhesus monkeys. Systemic administration of BU08028 (0.001-0.01 mg/kg) dose-dependently produced antinociception against acute thermal nociception and capsaicin-induced thermal allodynia. Compared to buprenorphine (0.01-0.1 mg/kg), the antinociceptive effect of BU08028 was more potent and much longer-lasting (i.e., more than 24 hours). BU08028-induced antinociception was attenuated equally by both mu opioid (MOP) receptor antagonist naltrexone (0.03 mg/kg) and NOP antagonist J-113397 (0.1 mg/kg), indicating that BU08028 is a bifunctional MOP/NOP agonist in primates. More importantly, BU08028 at antinociceptive doses did not compromise physiological functions including respiration and cardiovascular activities measured by the radio-telemetric probes. Compared to MOP agonists, buprenorphine and remifentanil, BU08028 did not produce reinforcing effects in monkeys under the progressive-ratio schedule of drug self-administration. These findings demonstrate that BU08028 potently produced long-lasting antinociception in the absence of common side effects associated with MOP agonists in primates. This study strongly supports the therapeutic potential of ligands with mixed MOP/NOP actions as innovative analgesics in humans (Supported by US-PHS grants DA-035359 and DA-032568).",
author = "Huiping Ding and Paul Czoty and Gerta Cami-Kobeci and Devki Sukhtankar and Michael Nader and Stephen Husbands and Mei-Chuan Ko",
year = "2015",
month = apr,
day = "1",
doi = "10.1096/fasebj.29.1_supplement.616.2",
language = "English",
volume = "29",
journal = "FASEB Journal",
issn = "0892-6638",
publisher = "FASEB",
number = "1",

}

RIS

TY - JOUR

T1 - BU08028 Displays a Promising Therapeutic Profile as an Analgesic in Monkeys

AU - Ding, Huiping

AU - Czoty, Paul

AU - Cami-Kobeci, Gerta

AU - Sukhtankar, Devki

AU - Nader, Michael

AU - Husbands, Stephen

AU - Ko, Mei-Chuan

PY - 2015/4/1

Y1 - 2015/4/1

N2 - BU08028, a novel buprenorphine analog, displays similar receptor binding profile like buprenorphine but with improved binding affinity and efficacy on nociceptin/orphanin FQ peptide (NOP) receptors. The aim of this study was to characterize the pharmacological profile of BU08028 as an analgesic in rhesus monkeys. Systemic administration of BU08028 (0.001-0.01 mg/kg) dose-dependently produced antinociception against acute thermal nociception and capsaicin-induced thermal allodynia. Compared to buprenorphine (0.01-0.1 mg/kg), the antinociceptive effect of BU08028 was more potent and much longer-lasting (i.e., more than 24 hours). BU08028-induced antinociception was attenuated equally by both mu opioid (MOP) receptor antagonist naltrexone (0.03 mg/kg) and NOP antagonist J-113397 (0.1 mg/kg), indicating that BU08028 is a bifunctional MOP/NOP agonist in primates. More importantly, BU08028 at antinociceptive doses did not compromise physiological functions including respiration and cardiovascular activities measured by the radio-telemetric probes. Compared to MOP agonists, buprenorphine and remifentanil, BU08028 did not produce reinforcing effects in monkeys under the progressive-ratio schedule of drug self-administration. These findings demonstrate that BU08028 potently produced long-lasting antinociception in the absence of common side effects associated with MOP agonists in primates. This study strongly supports the therapeutic potential of ligands with mixed MOP/NOP actions as innovative analgesics in humans (Supported by US-PHS grants DA-035359 and DA-032568).

AB - BU08028, a novel buprenorphine analog, displays similar receptor binding profile like buprenorphine but with improved binding affinity and efficacy on nociceptin/orphanin FQ peptide (NOP) receptors. The aim of this study was to characterize the pharmacological profile of BU08028 as an analgesic in rhesus monkeys. Systemic administration of BU08028 (0.001-0.01 mg/kg) dose-dependently produced antinociception against acute thermal nociception and capsaicin-induced thermal allodynia. Compared to buprenorphine (0.01-0.1 mg/kg), the antinociceptive effect of BU08028 was more potent and much longer-lasting (i.e., more than 24 hours). BU08028-induced antinociception was attenuated equally by both mu opioid (MOP) receptor antagonist naltrexone (0.03 mg/kg) and NOP antagonist J-113397 (0.1 mg/kg), indicating that BU08028 is a bifunctional MOP/NOP agonist in primates. More importantly, BU08028 at antinociceptive doses did not compromise physiological functions including respiration and cardiovascular activities measured by the radio-telemetric probes. Compared to MOP agonists, buprenorphine and remifentanil, BU08028 did not produce reinforcing effects in monkeys under the progressive-ratio schedule of drug self-administration. These findings demonstrate that BU08028 potently produced long-lasting antinociception in the absence of common side effects associated with MOP agonists in primates. This study strongly supports the therapeutic potential of ligands with mixed MOP/NOP actions as innovative analgesics in humans (Supported by US-PHS grants DA-035359 and DA-032568).

U2 - 10.1096/fasebj.29.1_supplement.616.2

DO - 10.1096/fasebj.29.1_supplement.616.2

M3 - Conference article

VL - 29

JO - FASEB Journal

JF - FASEB Journal

SN - 0892-6638

IS - 1

M1 - 616.2

ER -