Literature DB >> 9641560

The profile of sabcomeline (SB-202026), a functionally selective M1 receptor partial agonist, in the marmoset.

M H Harries1, N A Samson, J Cilia, A J Hunter.   

Abstract

1. Sabcomeline (SB-202026, 0.03 mg kg(-1), p.o.), a potent and functionally selective M1 receptor partial agonist, caused a statistically significant improvement in the performance of a visual object discrimination task by marmosets. No such improvement was seen after RS86 (0.1 mg kg(-1), p.o.). 2. Initial learning, which only required an association of object with reward and an appropriate response to be made, was not significantly affected. Reversal learning, which required both the extinction of the previously learned response and the acquisition of a new response strategy, was significantly improved after administration of sabcomeline (0.03 mg kg(-1), p.o.). 3. Sabcomeline (0.03 and 0.1 mg kg(-1), p.o.) had no significant effect on mean blood pressure measured for 2 h after administration in the conscious marmoset. 4. Sabcomeline (0.03 mg kg(-1), p.o.) caused none of the overt effects such as emesis or behaviours often seen after the administration of muscarinic agonists, e.g. face rubbing and licking. 5. This is the first study to demonstrate cognitive enhancement by a functionally selective M1 receptor partial agonist in a normal (i.e. non-cognitively impaired) non-human primate and this effect was seen at a dose which did not cause side effects. 6. Perseverative behaviour and deficient acquisition of new information are seen in patients with Alzheimer's disease (AD). Therefore the data suggest that sabcomeline might be of therapeutic benefit in the treatment of AD.

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Year:  1998        PMID: 9641560      PMCID: PMC1565397          DOI: 10.1038/sj.bjp.0701844

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  3 in total

1.  Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1.

Authors:  C J Langmead; N E Austin; C L Branch; J T Brown; K A Buchanan; C H Davies; I T Forbes; V A H Fry; J J Hagan; H J Herdon; G A Jones; R Jeggo; J N C Kew; A Mazzali; R Melarange; N Patel; J Pardoe; A D Randall; C Roberts; A Roopun; K R Starr; A Teriakidis; M D Wood; M Whittington; Z Wu; J Watson
Journal:  Br J Pharmacol       Date:  2008-05-05       Impact factor: 8.739

2.  Modulation of prepulse inhibition through both M(1) and M (4) muscarinic receptors in mice.

Authors:  Morgane Thomsen; Jürgen Wess; Brian S Fulton; Anders Fink-Jensen; S Barak Caine
Journal:  Psychopharmacology (Berl)       Date:  2009-12-15       Impact factor: 4.530

3.  Scopolamine Induces Deficits in Spontaneous Object-Location Recognition and Fear-Learning in Marmoset Monkeys.

Authors:  Jonathan L Melamed; Fernando M de Jesus; Rafael S Maior; Marilia Barros
Journal:  Front Pharmacol       Date:  2017-06-21       Impact factor: 5.810

  3 in total

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