Search Results - "Costa, Brian R."

Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting σ1 receptors produce anti-cocaine effects in mice by MATSUMOTO, Rae R, MCCRACKEN, Kari A, FRIEDMAN, Michele J, POUW, Buddy, DE COSTA, Brian R, BOWEN, Wayne D

Get full text

Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the .sigma. receptor by De Costa, Brian R, Radesca, Lilian, Di Paolo, Lisa, Bowen, Wayne D

“…By synthesizing and testing a part-structure, N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine (3), derived from our previously reported…”
Get full text

N-alkyl substituted analogs of the σ receptor ligand BD1008 and traditional σ receptor ligands affect cocaine-induced convulsions and lethality in mice by Matsumoto, Rae R., McCracken, Kari A., Pouw, Buddy, Miller, Jeffrey, Bowen, Wayne D., Williams, Wanda, De Costa, Brian R.

“…Cocaine binds to σ receptors with comparable affinity to its well-established interaction with dopamine transporters. Previous studies have shown BD1008 (…”
Get full text

Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity .sigma. receptor ligands by Radesca, Lilian, Bowen, Wayne D, Di Paolo, Lisa, De Costa, Brian R

“…N-Alkyl-substituted derivatives of (+)- and (-)-cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamin e have been synthesized in nine steps in a…”
Get full text

Subchronic administration of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine (BD1047) alters σ1 receptor binding by ZAMBON, A. C, DE COSTA, B. R, KANTHASAMY, A. G, NGUYEN, B. J. Q. H, MATSUMOTO, R. R

Get full text

Synthesis and Transporter Binding Properties of Bridged Piperazine Analogues of 1-{2-[Bis(4-fluorophenyl)methoxy]ethyl}-4-(3-phenylpropyl)piperazine (GBR 12909) by Zhang, Ying, Rothman, Richard B, Dersch, Christina M, de Costa, Brian R, Jacobson, Arthur E, Rice, Kenner C

“…A series of analogues related to 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2) and…”
Get full text

A new approach to the design of .sigma.-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine-related polyamines at .sigma.-1 and .sigma.-2 receptor subtypes by de Costa, Brian R, He, Xiao-shu, Dominguez, Celia, Cutts, Janet, Williams, Wanda, Bowen, Wayne D

“…A series of polyamines based on the high affinity sigma receptor ligand N-[2-(3,4-dichlorophenyl)-ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine (3) were…”
Get full text

Neuronal localization of cannabinoid receptors in the basal ganglia of the rat by Herkenham, M, Lynn, A B, de Costa, B R, Richfield, E K

“…Cannabinoid receptors have recently been characterized and localized using a high-affinity radiolabeled cannabinoid analog in section binding assays. In rat…”
Get more information

Differentiation of σ ligand‐activated receptor subtypes that modulate NMDA‐evoked [3H]‐noradrenaline release in rat hippocampal slices by Monnet, François P., Costa, Brian R., Bowen, Wayne D.

“…1 It is now widely accepted that there are two classes of sigma (σ) binding sites, denoted σ1 and σ2, and recently σ3 subtype has been proposed. Selective σ1…”
Get full text

Development of Novel, Potent, and Selective Dopamine Reuptake Inhibitors through Alteration of the Piperazine Ring of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) by Matecka, Dorota, Rothman, Richard B, Radesca, Lilian, de Costa, Brian R, Dersch, Christina M, Partilla, John S, Pert, Agu, Glowa, John R, Wojnicki, Francis H. E, Rice, Kenner C

“…The design, synthesis, and biological evaluation of compounds related to the dopamine (DA) uptake inhibitors: …”
Get full text

Apparent down-regulation of rat brain mu- and kappa-opioid binding sites labelled with [3H]cycloFOXY following chronic administration of the potent 5-hydroxytryptamine reuptake blocker, clomipramine by Benkelfat, C, Aulakh, C S, Bykov, V, Rice, K C, De Costa, B R, Rothman, R B

“…This study examined the effect of chronic clomipramine administration on opioid mu- and kappa-binding sites. Clomipramine (5 mg kg-1 day-1) or saline was…”
Get more information

Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors by Gu, Zi Qiang, Wong, Garry, Dominguez, Celia, de Costa, Brian R, Rice, Kenner C, Skolnick, Phil

“…A series of imidazo[1,5-a][1,4]benzodiazepine esters have been synthesized with varying ester side chains and 8-position substituents. The affinities of these…”
Get full text

Microinjection of sigma ligands into cranial nerve nuclei produces vacuous chewing in rats by TRAN, T. T, DE COSTA, B. R, MATSUMOTO, R. R

“…Many typical neuroleptics carry a high risk for producing motor side effects in humans, and have significant affinities for sigma (sigma) receptors. Sigma…”
Get full text

Interaction of endogenous opioid peptides and other drugs with four kappa opioid binding sites in guinea pig brain by Rothman, R B, Bykov, V, de Costa, B R, Jacobson, A E, Rice, K C, Brady, L S

“…Guinea pig brain membranes depleted of mu and delta receptors by pretreatment with the site-directed acylating agents, 2-(4-ethoxybenzyl)-1-…”
Get more information

Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at .sigma. receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds by de Costa, Brian R, He, Xiaoshu, Linders, Joannes T. M, Dominguez, Celia, Gu, Zi Qiang, Williams, Wanda, Bowen, Wayne

“…As a continuation of our earlier study (J. Med. Chem. 1992, 35, 4334-4343) we conformationally restricted the sigma-receptor ligand…”
Get full text

Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediamines as .sigma. receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes by De Costa, Brian R, Dominguez, Celia, He, Xiao Shu, Williams, Wanda, Radesca, Lilian, Bowen, Wayne

Get full text

Alterations in the stereochemistry of the .kappa.-selective opioid agonist U50,488 result in high-affinity .sigma. ligands by De Costa, Brian R, Bowen, Wayne D, Hellewell, Susan B, George, Clifford, Rothman, Richard B, Reid, Audrey A, Walker, J. Michael, Jacobson, Arthur E, Rice, Kenner C

“…The synthesis and in vitro sigma receptor activity of the two diastereomers of U50,488 [(+/-)-2], namely, (1R,2S)-(+)-…”
Get full text

Synthesis of N,N'-Substituted Piperazine and Homopiperazine Derivatives with Polyamine-like Actions at N-Methyl-D-aspartate Receptors by Zhou, Li-Ming, He, Xiao-Shu, Li, Guiying, de Costa, Brian R, Skolnick, Phil

“…A series of N,N'-substituted piperazine and homopiperazine derivatives have been synthesized with the objective of producing compounds that interact with…”
Get full text

Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites by He, Xiaoshu, Raymon, Lionel P, Mattson, Mariena V, Eldefrawi, Mohyee E, de Costa, Brian R

“…We previously reported (J. Med. Chem. 1993, 36, 1188-1193) that changes to the ring size of the piperidine and cyclohexyl rings of the high-affinity and…”
Get full text

Synthesis and binding characteristics of potential SPECT imaging agents for .sigma.-1 and .sigma.-2 binding sites by He, Xiao Shu, Bowen, Wayne D, Lee, Kan Sam, Williams, Wanda, Weinberger, Daniel R, De Costa, Brian R

“…2-, 3-, and 4-idophenyl derivatives of the high-affinity sigma ligand N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine (1) were…”
Get full text