ArticleBritish journal of pharmacology1993
Antinociceptive activity of NK1 receptor antagonists: non-specific effects of racemic RP67580.
Article in British journal of pharmacology, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 93 citations in OpenAlex.
- Opiranserin injection (Unafra®) as a first-in-class, non-opioid analgesic for the treatment of acute postoperative pain.Anesthesia and pain medicine · 2025Review
- The NK1 antagonist L-733,060 facilitates sequence learning.Journal of psychopharmacology (Oxford, England) · 2023Article
- Mechanical Conflict System: A Novel Operant Method for the Assessment of Nociceptive Behavior.PloS one · 2016Article
- Spinal or systemic TY005, a peptidic opioid agonist/neurokinin 1 antagonist, attenuates pain with reduced tolerance.British journal of pharmacology · 2010Article
- Neurokinin-1 receptors (NK1R:s), alcohol consumption, and alcohol reward in mice.Psychopharmacology · 2010Article
- In vivo evidence that protease-activated receptors 1 and 2 modulate gastrointestinal transit in the mouse.British journal of pharmacology · 2001Article
- Review
- Substance P and capsaicin-induced mechanical hyperalgesia in the rat knee joint; the involvement of bradykinin B1 and B2 receptors.British journal of pharmacology · 1996Article
- An isobolographic analysis of the effects of N-methyl-D-aspartate and NK1 tachykinin receptor antagonists on inflammatory hyperalgesia in the rat.British journal of pharmacology · 1996Article
- Antinociceptive activity of the tachykinin NK1 receptor antagonist, CP-99,994, in conscious gerbils.British journal of pharmacology · 1995Article
- Involvement of neurokinin receptors in the induction but not the maintenance of mechanical allodynia in rat flexor motoneurones.The Journal of physiology · 1995Article
- Central versus peripheral site of action of the tachykinin NK1-antagonist RP 67580 in inhibiting chemonociception.British journal of pharmacology · 1995Article
- Effect of the tachykinin NK1 receptor antagonists, RP 67580 and SR 140333, on electrically-evoked substance P release from rat spinal cord.British journal of pharmacology · 1994Article
- Blockade by oral or parenteral RPR 100893 (a non-peptide NK1 receptor antagonist) of neurogenic plasma protein extravasation within guinea-pig dura mater and conjunctiva.British journal of pharmacology · 1994Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Release of substance P in the dorsal horn is considered a primary event in the perception of pain. The profile of racemic RP67580, a non-peptide antagonist at the NK1 (substance P) receptor, was examined in a range of antinociception tests on rodents. 2. At doses up to 30 mg kg-1, s.c. racemic RP67580 exhibited antinociceptive activity in writhing and formalin paw tests in mice and gerbils. Acetic acid induced writhing and the licking response to formalin were reduced to 40-50% of the level observed in vehicle-treated animals (P < 0.05). However, this agent was not active in mouse tail flick, rat paw pressure or rat and guinea-pig formalin paw tests. 3. Like racemic RP67580, the calcium channel blockers nifedipine (30 mg kg-1, i.p.) and verapamil (10 or 20 mg kg-1, s.c.) inhibited the response to formalin by approximately 60% in gerbils (P < 0.05 compared with vehicle-treated animals). 4. Evidence for calcium channel antagonist activity of RP67580 was obtained in vitro. Racemic RP67580 inhibited calcium entry into depolarized strips of guinea-pig ileum longitudinal muscle myenteric plexus (apparent KB = 587 +/- 115 nM), inhibited [3H]-diltiazem binding to rabbit skeletal membranes (IC50 = 298 nM) and depressed high threshold calcium currents in neurones cultured from rat cortex (10% inhibition at 10 microM). 5. These findings indicate that the acute antinociceptive effects of RP67580 may not be attributable to a specific interaction with NK1 receptors and may be mediated via calcium channel blockade.
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