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PD 117302
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:111728-01-9
规格:≥98%

PD 117302 a new nonpeptide opioid compound shown in in vitro studies to be a selective kappa-opioid agonist, has been evaluated in vivo for antinociceptive activity and other effects characteristic of kappa-receptor activation. PD 117302 also causes naloxone-reversible locomotor impairment and diuresis, effects that are typical of kappa-agonists. It is an Anti-Arrhythmia Agent, an Anticonvulsants, a Cardiovascular Agent, and a Central Nervous System Agent. References: Leighton GE, Hill RG, Hughes J. The effects of the kappa agonist PD-117302 on feeding behaviour in obese and lean Zucker rats. Pharmacol Biochem Behav. 1988 Oct;31(2):425-9. PubMed PMID: 2854265. 2: Leighton GE, Johnson MA, Meecham KG, Hill RG, Hughes J. Pharmacological profile of PD 117302, a selective kappa-opioid agonist. Br J Pharmacol. 1987 Dec;92(4):915-22. PubMed PMID: 2827830; PubMed Central PMCID: PMC1853714. 3: Colombo M, Petrillo P, La Regina A, Bianchi G, Tavani A. In vitro binding profile and in vivo pharmacological properties of the K-opioid compound PD 117302. Res Commun Chem Pathol Pharmacol. 1991 Jun;72(3):295-306. PubMed PMID: 1658887. 4: Porreca F, Ianone M, Wheeler H, Cowan A. Comparison of PD 117302, a kappa agonist, and morphine on colonic transit and formalin-induced pain in rats. Proc West Pharmacol Soc. 1989;32:185-7. PubMed PMID: 2550944. 5: Pugsley MK, Saint DA, Hayes ES, Abraham S, Walker MJ. An examination of the cardiac actions of PD117,302, a κ-opioid receptor agonist. Eur J Pharmacol. 2015 Aug 15;76330-40. doi: 10.1016/j.ejphar.2015.06.018. Epub 2015 Jun 15. PubMed PMID: 26086860. 6: Moussaoui SM, Montier F, Carruette A, Blanchard JC, Laduron PM, Garret C. A non-peptide NK1-receptor antagonist, RP 67580, inhibits neurogenic inflammation postsynaptically. Br J Pharmacol. 1993 May;109(1):259-64. PubMed PMID: 7684305; PubMed Central PMCID: PMC2175579. 7: Parrott RF, Ebenezer IS, Baldwin BA, Forsling ML. Hormonal effects of apomorphine and cholecystokinin in pigs: modification of the response to cholecystokinin by a dopamine antagonist (metoclopramide) and a kappa opioid agonist (PD117302). Acta Endocrinol (Copenh). 1991 Oct;125(4):420-6. PubMed PMID: 1957561. 8: Shukla VK, Turndorf H, Bansinath M. Pertussis and cholera toxins modulate kappa-opioid receptor agonists-induced hypothermia and gut inhibition. Eur J Pharmacol. 1995 Mar 16;292(3-4):293-9. PubMed PMID: 7796869. 9: Wheeler-Aceto H, Cowan A. Standardization of the rat paw formalin test for the evaluation of analgesics. Psychopharmacology (Berl). 1991;104(1):35-44. PubMed PMID: 1882002. 10: Leighton GE, Hill RG, Hughes J. Effects of 5-HT and alpha 1 adrenoceptor antagonists on kappa opioid-induced sedation. Pharmacol Biochem Behav. 1988 Dec;31(4):899-904. PubMed PMID: 2855271. 1 Bansinath M, Ramabadran K, Turndorf H, Shukla VK. Intracerebroventricular administration of kappa-agonists induces convulsions in mice. Brain Res Bull. 1991 Jul;27(1):75-9. PubMed PMID: 1657321. 12: Nemmani KV, Gullapalli S, Ramarao P. Potentiation of kappa-opioid receptor agonist-induced analgesia and hypothermia by fluoxetine. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):189-93. PubMed PMID: 11420085. 13: Petrillo P, Kowalski J, Sbacchi M, Tavani A. Characterization of opioid binding sites in rat spinal cord. J Recept Res. 1992;12(1):39-57. PubMed PMID: 1314311. 14: Agbas A, Simon J, Avni Oktem H, Varga E, Borsodi A. Characterization of human placental opioid receptors by 3H-ethylketocyclazocine and 3H-naloxone binding. Neuropeptides. 1988 Oct;12(3):171-6. PubMed PMID: 2907370. 15: Carey GJ, Bergman J. Enadoline discrimination in squirrel monkeys: effects of opioid agonists and antagonists. J Pharmacol Exp Ther. 2001 Apr;297(1):215-23. PubMed PMID: 11259547. 16: Wilson JL, Walker JS, Antoon JS, Perry MA. Intercellular adhesion molecule-1 expression in adjuvant arthritis in rats: inhibition by kappa-opioid agonist but not by NSAID. J Rheumatol. 1998 Mar;25(3):499-505. PubMed PMID: 9517771. 17: Bansinath M, Ramabadran K, Turndorf H, Puig MM. Kappa-opiate agonist-induced inhibition of gastrointestinal transit in different strains of mice. Pharmacology. 1991;42(2):97-102. PubMed PMID: 1648236. 18: Gué M, Alvinerie M, Junien JL, Buéno L. Stimulation of kappa opiate receptors in intestinal wall affects stress-induced increase of plasma cortisol in dogs. Brain Res. 1989 Nov 13;502(1):143-8. PubMed PMID: 2555024. 19: Ribeiro W, Ifa DR, Corso G, Salmon J, Moraes LA, Eberlin MN, de Nucci G. Determination of RSD921 in human plasma by high-performance liquid chromatography-tandem mass spectrometry using tri-deuterated RSD921 as internal standard: application to a phase I clinical trial. J Mass Spectrom. 2001 Oct;36(10):1133-9. PubMed PMID: 11747107. 20: Sheridan RD. Quantification of state-dependent drug interactions with the sodium channel. Br J Pharmacol. 2000 Jan;129(2):409-11. PubMed PMID: 10694250; PubMed Central PMCID: PMC1571825.

纯度:≥98%

CAS:111728-01-9

 
 
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