Literature DB >> 10096443

The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors.

R H Mach1, L Wu, T West, B R Whirrett, S R Childers.   

Abstract

The analgesic properties of the tropane analogue (+/-)-SM 21 have been attributed to the antagonism of presynaptic m2 receptors resulting in a potentiation of acetylcholine release. However, drugs targeting a number of other neurotransmitter receptors have been shown to enhance acetylcholine release. In the current study, in vitro studies were conducted in order to determine the affinity of (+/-)-SM 21 for serotonin 5-HT3, 5-HT4, and sigma receptors. Our results indicate that (+/-)-SM 21, and its structural congeners, have a relatively high affinity for sigma2 receptors relative to their reported affinity for muscarinic receptors. The higher affinity for sigma2 versus sigma1 receptors indicates that (+/-)-SM 21 may be a suitable lead compound for developing sigma2-selective ligands.

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Year:  1999        PMID： 10096443     DOI： 10.1016/s0024-3205(99)00014-4

Source DB:  PubMed          Journal:  Life Sci        ISSN： 0024-3205            Impact factor:   5.037


  10 in total

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Review 5.  The σ2 receptor: a novel protein for the imaging and treatment of cancer.

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Authors:  Antonino N Fallica; Valeria Pittalà; Maria N Modica; Loredana Salerno; Giuseppe Romeo; Agostino Marrazzo; Mohamed A Helal; Sebastiano Intagliata
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10.  The Concise Guide to PHARMACOLOGY 2013/14: overview.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; John C McGrath; William A Catterall; Michael Spedding; John A Peters; Anthony J Harmar; N Abul-Hasn; C M Anderson; C M H Anderson; M S Araiksinen; M Arita; E Arthofer; E L Barker; C Barratt; N M Barnes; R Bathgate; P M Beart; D Belelli; A J Bennett; N J M Birdsall; D Boison; T I Bonner; L Brailsford; S Bröer; P Brown; G Calo; W G Carter; W A Catterall; S L F Chan; M V Chao; N Chiang; A Christopoulos; J J Chun; J Cidlowski; D E Clapham; S Cockcroft; M A Connor; H M Cox; A Cuthbert; F M Dautzenberg; A P Davenport; P A Dawson; G Dent; J P Dijksterhuis; C T Dollery; A C Dolphin; M Donowitz; M L Dubocovich; L Eiden; K Eidne; B A Evans; D Fabbro; C Fahlke; R Farndale; G A Fitzgerald; T M Fong; C J Fowler; J R Fry; C D Funk; A H Futerman; V Ganapathy; B Gaisnier; M A Gershengorn; A Goldin; I D Goldman; A L Gundlach; B Hagenbuch; T G Hales; J R Hammond; M Hamon; J C Hancox; R L Hauger; D L Hay; A J Hobbs; M D Hollenberg; N D Holliday; D Hoyer; N A Hynes; K-I Inui; S Ishii; K A Jacobson; G E Jarvis; M F Jarvis; R Jensen; C E Jones; R L Jones; K Kaibuchi; Y Kanai; C Kennedy; I D Kerr; A A Khan; M J Klienz; J P Kukkonen; J Y Lapoint; R Leurs; E Lingueglia; J Lippiat; S J Lolait; S C R Lummis; J W Lynch; D MacEwan; J J Maguire; I L Marshall; J M May; C A McArdle; J C McGrath; M C Michel; N S Millar; L J Miller; V Mitolo; P N Monk; P K Moore; A J Moorhouse; B Mouillac; P M Murphy; R R Neubig; J Neumaier; B Niesler; A Obaidat; S Offermanns; E Ohlstein; M A Panaro; S Parsons; R G Pwrtwee; J Petersen; J-P Pin; D R Poyner; S Prigent; E R Prossnitz; N J Pyne; S Pyne; J G Quigley; R Ramachandran; E L Richelson; R E Roberts; R Roskoski; R A Ross; M Roth; G Rudnick; R M Ryan; S I Said; L Schild; G J Sanger; K Scholich; A Schousboe; G Schulte; S Schulz; C N Serhan; P M Sexton; D R Sibley; J M Siegel; G Singh; R Sitsapesan; T G Smart; D M Smith; T Soga; A Stahl; G Stewart; L A Stoddart; R J Summers; B Thorens; D T Thwaites; L Toll; J R Traynor; T B Usdin; R J Vandenberg; C Villalon; M Vore; S A Waldman; D T Ward; G B Willars; S J Wonnacott; E Wright; R D Ye; A Yonezawa; M Zimmermann
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  10 in total

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