Tolerance and dependence following chronic intracerebroventricular infusions of Tyr-D-Arg2-Phe-Sar4 (TAPS)
| Autor: | Bijal D Gudka, Anna-Leena Sirén, Stefan Vonhof |
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| Rok vydání: | 2002 |
| Předmět: |
Male
medicine.medical_specialty Time Factors Enkephalin Substance-Related Disorders Pain In Vitro Techniques Rats Sprague-Dawley 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Bolus (medicine) Internal medicine Medicine Animals Receptor Infusion Pumps 030304 developmental biology Injections Intraventricular Pharmacology 0303 health sciences Tetrapeptide Dose-Response Relationship Drug Morphine business.industry Naloxone Dermorphin Drug Tolerance Enkephalin Ala(2)-MePhe(4)-Gly(5) 3. Good health Rats Substance Withdrawal Syndrome Analgesics Opioid DAMGO Nociception Endocrinology chemistry Mechanism of action medicine.symptom business Oligopeptides 030217 neurology & neurosurgery |
| Zdroj: | European journal of pharmacology. 459(1) |
| ISSN: | 0014-2999 |
| Popis: | The dermorphin-derived tetrapeptide Tyr- d -Arg 2 -Phe-Sar 4 (TAPS) was tested for its ability to induce tolerance, cross-tolerance, withdrawal and its substitution properties in rats subjected to chronic intracerebroventricular (i.c.v.) infusions of μ-opiate receptor agonists. Tolerance and cross-tolerance were assessed by quantification of the thermally induced tail-flick response. Chronic intracerebroventricular infusion of TAPS resulted in antinociception at almost 1000-fold lower doses compared to morphine sulphate and [ d -Ala 2 , MePhe 4 Gly(ol) 5 ]enkephalin (DAMGO). Tolerance to the antinociceptive effect of TAPS developed similar to DAMGO and morphine sulphate. Cross-tolerance to intracerebroventricular bolus injections of DAMGO, but not of TAPS, was evident in rats rendered tolerant to morphine sulphate and TAPS. Naloxone-induced withdrawal was equally pronounced in animals treated with morphine sulphate, DAMGO or TAPS. TAPS substituted for morphine sulphate and vice versa regarding the withdrawal syndrome in a cross-over experimental design. In contrast to DAMGO, TAPS retains its antinociceptive effect following bolus administration in rats rendered tolerant to μ-opioid receptor agonists. |
| Databáze: | OpenAIRE |
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