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Small constrained S...
Small constrained SP1-7 analogues bind to a unique site and promote anti-allodynic effects following systemic injection in mice
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- Jonsson, Anna, 1981- (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap,Biologisk beroendeforskning
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- Fransson, Rebecca (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Haramaki, Yutaka (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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- Skogh, Anna (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Brolin, Erika (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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- Watanabe, Hiroyuki (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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Nordvall, Gunnar (author)
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- Hallberg, Mathias (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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- Sandström, Anja (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Nyberg, Fred (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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(creator_code:org_t)
- Elsevier BV, 2015
- 2015
- English.
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In: Neuroscience. - : Elsevier BV. - 0306-4522 .- 1873-7544. ; 298, s. 112-119
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Previous results have shown that the substance P (SP) N-terminal fragment SP1–7 may attenuate hyperalgesia and produce anti-allodynia in animals using various experimental models for neuropathic pain. The heptapeptide was found to induce its effects through binding to and activating specific sites apart from any known neurokinin or opioid receptor. Furthermore, we have applied a medicinal chemistry program to develop lead compounds mimicking the effect of SP1–7. The present study was designed to evaluate the pharmacological effect of these compounds using the mouse spared nerve injury (SNI) model of chronic neuropathic pain. Also, as no comprehensive screen with the aim to identify the SP1–7 target has yet been performed we screened our lead compound H-Phe-Phe-NH2 toward a panel of drug targets. The extensive target screen, including 111 targets, did not reveal any hit for the binding site among a number of known receptors or enzymes involved in pain modulation. Our animal studies confirmed that SP1–7, but also synthetic analogs thereof, possesses anti-allodynic effects in the mouse SNI model of neuropathic pain. One of the lead compounds, a constrained H-Phe-Phe-NH2 analog, was shown to exhibit a significant anti-allodynic effect.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Jonsson, Anna, 1 ...
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Fransson, Rebecc ...
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Haramaki, Yutaka
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Skogh, Anna
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Brolin, Erika
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Watanabe, Hiroyu ...
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show more...
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Nordvall, Gunnar
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Hallberg, Mathia ...
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Sandström, Anja
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Nyberg, Fred
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmaceutical S ...
- Articles in the publication
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Neuroscience
- By the university
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Uppsala University