Cited by 141Neuropeptides and Animal PhysiologyReceptor Mechanisms and SignalingNeurotransmitter Receptor Influence on Behavior

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Buprenorphine has potent kappa opioid receptor antagonist activity

LEANDER, J·1987·Neuropharmacology

DOI 10.1016/0028-3908(87)90112-2

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Abstract

Buprenorphine was studied for its effects on urinary output to determine if it was an agonist, partial agonist, or antagonist at the kappa receptor. Buprenorphine was a potent antagonist of bremazocine-induced urination and had no kappa agonist activity. Thus, the high affinity that buprenorphine has for the kappa receptor results in potent kappa receptor antagonist activity in vivo.

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Authors: LEANDER, J.
Affiliations: Eli Lilly (United States) (US)
Corresponding author: LEANDER, J
ORCID: LEANDER, J
Venue: Neuropharmacology
Publisher: Elsevier BV
Published: 1987-09
Volume: 26
Issue: 9
Pages: 1445-1447
ISSN: 0028-3908 (ISSN-L)
DOI: 10.1016/0028-3908(87)90112-2
OpenAlex: W2146835843
Cited by: 140
References: 8
Citations by year: 2025: 3 · 2024: 3 · 2023: 2 · 2022: 6 · 2021: 2 · 2020: 3 · 2019: 2 · 2018: 13 · 2017: 1 · 2016: 3 · 2015: 1 · 2014: 9 · 2013: 2 · 2012: 5
FWCI: 0.69
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Neuropharmacology (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
Keywords: buprenorphine, kappa opioid receptor, receptor antagonism, partial agonist activity, bremazocine, urine output, opioid receptor affinity
MeSH terms: Animals, Benzomorphans, Buprenorphine, Diuresis, Drug Combinations, Male, Naltrexone, Rats, Inbred Strains, Receptors, Opioid, Rats

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Buprenorphine has potent kappa opioid receptor antagonist activity

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