BD1063
Chemical compound
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ECHA InfoCard | 100.229.843 |
Chemical and physical data | |
Formula | C13H18Cl2N2 |
Molar mass | 273.20 g·mol−1 |
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BD1063 or 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity over the sigma-2 receptor.[1]
Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine.[1]
In other animal studies, BD1063 blocks the effects of MDMA,[2] and reduces alcohol intake in rodent models of alcoholism.[3]
See also
- BD1008
- BD1031
- LR132
References
- ^ a b Matsumoto RR, McCracken KA, Friedman MJ, Pouw B, De Costa BR, Bowen WD (2001). "Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice". Eur. J. Pharmacol. 419 (2–3): 163–74. doi:10.1016/s0014-2999(01)00968-2. PMID 11426838.
- ^ Brammer MK, Gilmore DL, Matsumoto RR (December 2006). "Interactions between 3,4-methylenedioxymethamphetamine and sigma1 receptors". European Journal of Pharmacology. 553 (1–3): 141–5. doi:10.1016/j.ejphar.2006.09.038. PMC 1780037. PMID 17070798.
- ^ Sabino V, Cottone P, Zhao Y, Iyer MR, Steardo L, Steardo L, Rice KC, Conti B, Koob GF, Zorrilla EP (May 2009). "The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking". Neuropsychopharmacology. 34 (6): 1482–93. doi:10.1038/npp.2008.192. PMC 2669694. PMID 18946467.
- v
- t
- e
- Agonists: 3-PPP
- 4-PPBP
- 5-MeO-DMT
- Alazocine (SKF-10047)
- Amantadine
- Arketamine
- BD-737
- BD-1052
- Blarcamesine
- Captodiame
- Citalopram
- CGRPTooltip Calcitonin gene-related peptide
- Cloperastine
- Cocaine
- Cutamesine (SA-4503)
- Cyclazocine
- Dehydroepiandrosterone (DHEA) (prasterone)
- Dehydroepiandrosterone sulfate (DHEA-S) (prasterone sulfate)
- Dextrallorphan
- Dextromethorphan (DXM)
- Dextrorphan (DXO)
- Dimemorfan
- Dimethyltryptamine (DMT)
- Ditolylguanidine (DTG)
- Donepezil
- Eliprodil
- Escitalopram
- Fabomotizole (afobazole)
- Fluoxetine
- Fluvoxamine
- Ifenprodil
- Igmesine (JO-1784)
- IPAB
- Ketamine
- L-687384
- MDMA (midomafetamine)
- Memantine
- Methamphetamine
- Methoxetamine
- Methylphenidate
- Nepinalone
- Neuropeptide Y
- Noscapine
- OPC-14523
- Opipramol
- Pentazocine
- Pentoxyverine (carbetapentane)
- PRE-084
- Pregnenolone
- Pregnenolone sulfate
- Pridopidine
- Racemethorphan (methorphan)
- Racemorphan (morphanol)
- UMB-23
- UMB-82
- Antagonists: 3-PPP
- AC-927
- BD-1008
- BD-1031
- BD-1047
- BD-1060
- BD-1063
- BD-1067
- BMY-14802 (BMS-181100)
- CM-156
- Dup-734
- E-5842
- E-52862 (S1RA)
- Haloperidol
- LR-132
- LR-172
- MS-377
- NE-100
- NPC-16377
- Panamesine (EMD-57455)
- PD-144418
- Pentazocine
- Progesterone
- Rimcazole (BW-234U)
- Sertraline
- SR-31742A
- Allosteric modulators: Phenytoin; Positive: Methylphenylpiracetam
- SOMCL-668
- Unknown/unsorted: 3-Methoxydextrallorphan
- 3-MeO-PCP
- 4C-T-2
- 4-IBP
- 4-IPBS
- 4-MeO-PCP
- 5-MeO-DALT
- 5-MeO-DiPT
- Amitriptyline
- Azidopamil
- Chlorpromazine
- Clemastine
- Clomipramine
- Clorgiline
- D-Deprenyl
- DiPTTooltip N,N-Diisopropyltryptamine
- DPTTooltip N,N-Dipropyltryptamine
- Ibogaine
- Imipramine
- KCR-12-83.1
- Nemonapride
- Noribogaine
- RHL-033
- RS-67,333
- RTI-55
- Saffron
- Safinamide
- Selegiline
- Spipethiane
- Trifluoperazine
- W-18
- YKP10A
- Agonists: 3-PPP
- Arketamine
- BD-1047
- BD1063
- Ditolylguanidine (DTG)
- DKR-1005
- DKR-1051
- Haloperidol
- Ifenprodil
- Ketamine
- MDMA (midomafetamine)
- Methamphetamine
- OPC-14523
- Opipramol
- PB-28
- Phencyclidine
- Siramesine (Lu 28-179)
- UKH-1114
- Unknown/unsorted: 3-Methoxydextrallorphan
- 3-MeO-PCE
- 4-MeO-PCP
- 5-MeO-DALT
- 5-MeO-DiPT
- Clemastine
- DiPTTooltip N,N-Diisopropyltryptamine
- DPTTooltip N,N-Dipropyltryptamine
- Ibogaine
- Nemonapride
- Nepinalone
- Noribogaine
- Pentazocine
- RS-67,333
- Safinamide
- TMATooltip 3,4,5-Trimethoxyamphetamine
- UMB-23
- UMB-82
- W-18
- Antagonists: AHD1
- AZ66
- Lamotrigine
- Naloxone
- SM-21
- UMB-100
- UMB-101
- UMB-103
- UMB-116
- YZ-011
- YZ-069
- YZ-185
- Allosteric modulators: SKF-83959
- Unknown/unsorted: 18-Methoxycoronaridine
- BMY-13980
- Butaclamol
- Caramiphen
- Carvotroline
- Chlorphenamine (chlorpheniramine)
- Chlorpromazine
- Cinnarizine
- Cinuperone
- Clocapramine
- Dezocine
- EMD-59983
- Hypericin (St. John's wort)
- Fluphenazine
- Gevotroline (WY-47384)
- Mepyramine (pyrilamine)
- Molindone
- Perphenazine
- Pimozide
- Proadifen
- Promethazine
- Propranolol
- Quinidine
- Remoxipride
- SL 82.0715
- SR-31747A
- Tiospirone (BMY-13859)
- Venlafaxine
See also: Receptor/signaling modulators