N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects

Daniels, AnTawan; Ayala, Erika; Chen, Weibin; Coop, Andrew; Matsumoto, Rae R.

doi:10.1016/j.ejphar.2006.03.062

Cited by 9 publications

(16 citation statements)

References 42 publications

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“…These dose-dependent rightward shifts produced by CocE are profound. No other reported agents are able to shift the dose-response curve for cocaine toxicity to this extent (Gasior et al, 2000;Carrera et al, 2005;Daniels et al, 2006). These findings further support the first in vivo study of CocE in rats demonstrating CocE's rapid and robust protection against cocaine-induced lethality (Cooper et al, 2006).…”

Section: Discussionsupporting

confidence: 75%

“…Cocaine-induced toxicity was characterized by the occurrence of convulsions and lethality. Cocaine-induced convulsions were defined as loss of righting posture for at least 5 s with the simultaneous presence of clonic limb movements (Gasior et al, 2000;Daniels et al, 2006). Lethality was defined as cessation of observed movement and respiration.…”

Section: Methodsmentioning

confidence: 99%

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Cocaine Esterase: Interactions with Cocaine and Immune Responses in Mice

Ko¹,

Bowen²,

Narasimhan³

et al. 2007

The Journal of Pharmacology and Experimental Therapeutics

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Section: Discussionsupporting

confidence: 75%

Section: Methodsmentioning

confidence: 99%

Cocaine Esterase: Interactions with Cocaine and Immune Responses in Mice

Ko¹,

Bowen²,

Narasimhan³

et al. 2007

The Journal of Pharmacology and Experimental Therapeutics

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“…However, few s 1 -selective ligands are presently available, and BD1047, which has nanomolar affinity for the s 1 receptor, is the most selective and potent s 1 receptor antagonist described to date (Daniels et al, 2006;Matsumoto et al, 1995;McCracken et al, 1999a, b). Moreover, although BD1047 also has moderate affinity for s 2 receptors and b-adrenergic receptors, it shows substantial selectivity for s 1 receptors (E50 times over s 2 receptors, and E150 times over b-adrenergic receptors), providing confidence that, at the dose range used, the behavioral effects obtained here are attributable to an action at s 1 receptors (Matsumoto et al, 1995).…”

Section: Discussionmentioning

confidence: 99%

Differential Effects of σ1 Receptor Blockade on Self-Administration and Conditioned Reinstatement Motivated by Cocaine vs Natural Reward

Martin‐Fardon

Maurice

Aujla

et al. 2007

Neuropsychopharmacol

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Growing evidence suggests a role for sigma 1 (s 1 ) receptors in cognitive function, anxiety, depression, regulation of stress responses, and, recently, the appetitive effects of cocaine as measured by conditioned place preference. This study was designed to extend understanding of the role of s 1 receptors in addiction-relevant conditioned effects of cocaine by testing the effects of a potent and selective s 1 receptor antagonist, BD1047, on conditioned reinstatement of cocaine-seeking. To determine whether modification of conditioned reinstatement by BD1047 is selective for drug-directed behavior or reflects general suppressant effects on motivated behavior, BD1047 was tested also on reinstatement induced by stimuli conditioned to a natural reward, sweetened condensed milk (SCM). Additionally, because s 1 receptors have been implicated also in processes linked to the acute reinforcing actions of cocaine, tests of the effects of BD1047 on cocaine self-administrationFincluding a comparison with the s 1 antagonist effects on SCM self-administrationFwere conducted as well. Cocaine self-administering male Wistar rats were trained to associate a discriminative stimulus (S D ) with the availability of cocaine or SCM, and then subjected to reinstatement tests following extinction of cocaine or SCM-reinforced behavior. BD1047 (1-30 mg/kg) reversed response reinstatement induced by the cocaine S D at 20 and 30 mg/kg but did not modify SCM S D -induced responding at all but the highest 30 mg dose, at which responding was reversed to extinction levels. BD1047 did not modify responding reinforced directly by SCM or cocaine. The findings support a role for s 1 receptors in regulating conditioned responses to cocaine-related contextual stimuli and identify this receptor as a potential treatment target for the prevention of craving and relapse.

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“…To study the effect of ring size and N-alkyl susbstituents on anti-cocaine activity, UMB115-117 ( Table 11) with five membered pyrrolidine ring system were evaluated [137].…”

Section: Bd1018mentioning

confidence: 99%

Sigma Receptors and Cocaine Abuse

Narayanan¹,

Mésangeau²,

Poupaert³

et al. 2011

CTMC

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Sigma receptors have been well documented as a protein target for cocaine and have been shown to be involved in the toxic and stimulant actions of cocaine. Strategies to reduce the access of cocaine to sigma receptors have included antisense oligonucleotides to the sigma-1 receptor protein as well as small molecule ligand with affinity for sigma receptor sites. These results have been encouraging as novel protein targets that can attenuate the actions of cocaine are desperately needed as there are currently no medications approved for treatment of cocaine toxicity or addiction. Many years of research in this area have yet to produce an effective treatment and much focus was on dopamine systems. A flurry of research has been carried out to elucidate the role of sigma receptors in the blockade of cocaine effects but this research has yet to yield a clinical agent. This review summarizes the work to date on the linkage of sigma receptors and the actions of cocaine and the progress that has been made with regard to small molecules. Although there is still a lack of an agent in clinical trials with a sigma receptor mechanism of action, work is progressing and the ligands are becoming more selective for sigma systems and the potential remains high.

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N-[2-(m-methoxyphenyl)ethyl]-N-ethyl-2-(1-pyrrolidinyl)ethylamine (UMB 116) is a novel antagonist for cocaine-induced effects

Cited by 9 publications

References 42 publications

Cocaine Esterase: Interactions with Cocaine and Immune Responses in Mice

Cocaine Esterase: Interactions with Cocaine and Immune Responses in Mice

Differential Effects of σ1 Receptor Blockade on Self-Administration and Conditioned Reinstatement Motivated by Cocaine vs Natural Reward

Sigma Receptors and Cocaine Abuse

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