BD 1008 dihydrobromide - CAS 138356-09-9
Category: Inhibitor
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Sigma Receptor
BD 1008 dihydrobromide is a potent and selective σ receptor antagonist displaying 4-fold selectivity for σ1 over σ2. BD-1008 attenuates the toxicity and stimulant effects of cocaine, and can be used as the treatment of cocaine overdose and neuropathic pain after chemotherapy.
Brife Description:
σ receptor antagonist
N-[2-(3,4-Dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine dihydrobromide; 2-(3,4-dichlorophenyl)-N-methyl-N-(2-pyrrolidin-1-ylethyl)ethanamine dihydrobromide
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1.Decreases in cocaine self-administration with dual inhibition of the dopamine transporter and σ receptors.
Hiranita T;Soto PL;Kohut SJ;Kopajtic T;Cao J;Newman AH;Tanda G;Katz JL J Pharmacol Exp Ther. 2011 Nov;339(2):662-77. doi: 10.1124/jpet.111.185025. Epub 2011 Aug 22.
Sigma receptor (σR) antagonists attenuate many behavioral effects of cocaine but typically not its reinforcing effects in self-administration procedures. However, the σR antagonist rimcazole and its N-propylphenyl analogs, [3-(cis-3,5-dimethyl-4-[3-phenylpropyl]-1-piperazinyl)-propyl]diphenylamine hydrochloride (SH 3-24) and 9-[3-(cis-3,5-dimethyl-4-[3-phenylpropyl]-1-piperazinyl)-propyl]carbazole hydrobromide (SH 3-28), dose-dependently decreased the maximal rates of cocaine self-administration without affecting comparable responding maintained by food reinforcement. In contrast, a variety of σR antagonists [N-phenethylpiperidine oxalate (AC927), N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine dihydrobromide (BD 1008), N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino) ethylamine dihydrobromide (BD 1047), N-[2-(3,4-dichlorophenyl) ethyl]-4-methylpiperazine dihydrochloride (BD 1063), and N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride (NE-100)] had no effect on cocaine self-administration across the range of doses that decreased rates of food-maintained responding. Rimcazole analogs differed from selective σR antagonists in their dual affinities for σRs and the dopamine transporter (DAT) assessed with radioligand binding.
2.Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist.
Desai RI;Grandy DK;Lupica CR;Katz JL J Pharmacol Exp Ther. 2014 Jan;348(1):106-15. doi: 10.1124/jpet.113.208538. Epub 2013 Nov 5.
An N-butyl analog of benztropine, JHW007 [N-(n-butyl)-3α-[bis(4'-fluorophenyl)methoxy]-tropane], binds to dopamine transporters (DAT) but has reduced cocaine-like behavioral effects and antagonizes various effects of cocaine. The present study further examined mechanisms underlying these effects. Cocaine dose-dependently increased locomotion, whereas JHW007 was minimally effective but increased activity 24 hours after injection. JHW007 (3-10 mg/kg) dose-dependently and fully antagonized the locomotor-stimulant effects of cocaine (5-60 mg/kg), whereas N-methyl and N-allyl analogs and the dopamine (DA) uptake inhibitor GBR12909 [1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride] stimulated activity and failed to antagonize effects of cocaine. JHW007 also blocked the locomotor-stimulant effects of the DAT inhibitor GBR12909 but not stimulation produced by the δ-opioid agonist SNC 80 [4-[(R)-[(2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl](3-methoxyphenyl)methyl]-N,N-diethylbenzamide], which increases activity through nondopaminergic mechanisms. JHW007 blocked locomotor-stimulant effects of cocaine in both DA D2- and CB1-receptor knockout and wild-type mice, indicating a lack of involvement of these targets.
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CAS 138356-09-9 BD 1008 dihydrobromide

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