138356-09-9
Chemical Structure
BD-1008 dihydrobromide
- CAS No.: 138356-09-9
- Formula:C15H24Br2Cl2N2
- Molecular Weight:463.08
IUPAC Name: N-(3,4-dichlorophenethyl)-N-methyl-2-(pyrrolidin-1-yl)ethan-1-amine dihydrobromide
InChIKey: YTBUMHOSKIAYCZ-UHFFFAOYSA-N
SMILES: CN(CCC1=CC=C(Cl)C(Cl)=C1)CCN2CCCC2.Br.Br
Biological Activity: BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor[1][2][3].
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BD-1008 dihydrobromide | 98.07% | BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor. | ||||||||||||||||||||
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BD-1008-d5 dihydrobromide | BD-1008-d5 dihydrobromide is the deuterium labeled BD-1008 dihydrobromide (HY-100966). BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor. | |||||||||||||||||||||
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- [1]. Staelens L, et al. In vivo evaluation of [(123)I]-3-(4-iodobenzyl)-1,2,3,4-tetrahydro-8-hydroxychromeno[3,4-c]pyridin-5-one: a presumed dopamine D4 receptor ligand for SPECT studies. Nucl Med Biol. 2005 Apr;32(3):293-9. [Content Brief]
- [2]. Garcés-Ramírez L, et al. Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis. Biol Psychiatry. 2011 Feb 1;69(3):208-17. [Content Brief]
- [3]. Hiranita T, et al. Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats. J Pharmacol Exp Ther. 2013 Oct;347(1):20-9. [Content Brief]
