2006
DOI: 10.1038/sj.npp.1301189
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SSR180711, a Novel Selective α7 Nicotinic Receptor Partial Agonist: (1) Binding and Functional Profile

Abstract: In this paper, we report on the pharmacological and functional profile of SSR180711 (1,4-Diazabicyclo[3.2.2]nonane-4-carboxylic acid, 4-bromophenyl ester), a new selective a7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 displays high affinity for rat and human a7 n-AChRs (K i of 2274 and 1471 nM, respectively). Ex vivo 3 [H]a-bungarotoxin binding experiments demonstrate that SSR180711 rapidly penetrates into the brain (ID 50 ¼ 8 mg/kg p.o.). In functional studies performed with human a… Show more

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Cited by 169 publications
(115 citation statements)
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“…Alternatively, the capacity of SSR180711 to restore disrupted LI may stem from an action that is unrelated to dopaminergic function. One possibility is that SSR180711 restores LI by increasing frontal ACh levels (Biton et al, 2007), because such an increase is expected to facilitate attentional processing (Hasselmo and McGaughy, 2004;Sarter and Bruno, 2000) through both nicotinic and muscarinic receptors (Hasselmo, 2006;Hasselmo and McGaughy, 2004). In this case, a7 partial agonism would be expected to target positive symptoms directly through modulation of aberrant stimulus salience.…”
Section: Reversal Of Disrupted Li: Putative Efficacy For Positive Symmentioning
confidence: 99%
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“…Alternatively, the capacity of SSR180711 to restore disrupted LI may stem from an action that is unrelated to dopaminergic function. One possibility is that SSR180711 restores LI by increasing frontal ACh levels (Biton et al, 2007), because such an increase is expected to facilitate attentional processing (Hasselmo and McGaughy, 2004;Sarter and Bruno, 2000) through both nicotinic and muscarinic receptors (Hasselmo, 2006;Hasselmo and McGaughy, 2004). In this case, a7 partial agonism would be expected to target positive symptoms directly through modulation of aberrant stimulus salience.…”
Section: Reversal Of Disrupted Li: Putative Efficacy For Positive Symmentioning
confidence: 99%
“…Although little is known on the effects of SSR180711 on mesolimbic DA dynamics (Hansen et al, 2007), it seems unlikely that this agent would directly block NAC DA increase, given the well known action of nicotine to increase DA release in the NAC (Wonnacott et al, 2005), an effect blocked by a7 antagonists (Schilstrom et al, 1998(Schilstrom et al, , 2000. The capacity of SSR180711 to increase glutamate neurotransmission in the hippocampus as well as increase dopamine levels in the PFC (Biton et al, 2007;Pichat et al, 2007) could underlie reversal of amphetamine-induced disruption and potentiation of LI, since both would be expected to reduce mesolimbic DA function and block behavioral effects of amphetamine Grace, 2005, 2007;Grace, 1991;Jackson and Moghaddam, 2001). Alternatively, the capacity of SSR180711 to restore disrupted LI may stem from an action that is unrelated to dopaminergic function.…”
Section: Reversal Of Disrupted Li: Putative Efficacy For Positive Symmentioning
confidence: 99%
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