Literature DB >> 2812509

(+-)-cis-2-methyl-spiro(1,3-oxathiolane-5,3') quinuclidine (AF102B): a new M1 agonist attenuates cognitive dysfunctions in AF64A-treated rats.

A Fisher1, R Brandeis, Z Pittel, I Karton, M Sapir, S Dachir, A Levy, E Heldman.   

Abstract

(+-)-cis-2-Methyl-spiro(1,3-oxathiolane-5,3')quinuclidine (AF102B), a new muscarinic agonist of utmost rigidity, exhibits a high selectivity for M1 muscarinic receptors. In rats having a cholinergic hypofunction induced by the intracerebroventricular administration of ethylcholine aziridinium (AF64A), AF102B reversed cognitive impairments in a step-through passive avoidance task and in an 8-arm radial maze. AF102B reversed cognitive impairments at significantly lower doses than those needed to induce side-effects. In addition, AF102B exhibited low toxicity. The results suggest that AF102B may prove useful for treatments of cholinergic deficiencies and cognitive impairments, like those reported in Alzheimer's disease.

Entities:  

Mesh：

Substances：

Year:  1989        PMID： 2812509     DOI： 10.1016/0304-3940(89)90100-6

Source DB:  PubMed          Journal:  Neurosci Lett        ISSN： 0304-3940            Impact factor:   3.046


  7 in total

Review 1.  Behavioral screening for cognition enhancers: from indiscriminate to valid testing: Part I.

Authors:  M Sarter; J Hagan; P Dudchenko
Journal:  Psychopharmacology (Berl)       Date:  1992       Impact factor: 4.530

2.  Protection against developmental deficiencies by a lipophilic VIP analogue.

Authors:  I Gozes; M Bachar; A Bardea; A Davidson; S Rubinraut; M Fridkin
Journal:  Neurochem Res       Date:  1998-05       Impact factor: 3.996

3.  Mapping the active site in vasoactive intestinal peptide to a core of four amino acids: neuroprotective drug design.

Authors:  I Gozes; O Perl; E Giladi; A Davidson; O Ashur-Fabian; S Rubinraut; M Fridkin
Journal:  Proc Natl Acad Sci U S A       Date:  1999-03-30       Impact factor: 11.205

4.  SDZ ENS 163 is a selective M1 agonist and induces release of acetylcholine.

Authors:  A Enz; G Shapiro; P Supavilai; H W Boddeke
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-03       Impact factor: 3.000

5.  Review of the Pharmacological Properties and Clinical Usefulness of Muscarinic Agonists for Xerostomia in Patients with Sjögren's Syndrome.

Authors:  Hiroshi Yasuda; Hiroshi Niki
Journal:  Clin Drug Investig       Date:  2002       Impact factor: 2.859

6.  Role of muscarinic receptor subtypes in central antinociception.

Authors:  A Bartolini; C Ghelardini; L Fantetti; M Malcangio; P Malmberg-Aiello; A Giotti
Journal:  Br J Pharmacol       Date:  1992-01       Impact factor: 8.739

7.  Neuroprotective strategy for Alzheimer disease: intranasal administration of a fatty neuropeptide.

Authors:  I Gozes; A Bardea; A Reshef; R Zamostiano; S Zhukovsky; S Rubinraut; M Fridkin; D E Brenneman
Journal:  Proc Natl Acad Sci U S A       Date:  1996-01-09       Impact factor: 11.205
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.