Autoradiographic identification and characterization of σ receptors in guinea pig brain using [3H]1(cyclopropylmethyl)-4-(2′-(4≈-fluorophenyl)-2′-oxoethyl) piperidine ([3H]DuP 734), a novel σ receptor ligand

Heroux, Jeffrey A.; Tam, S. William; Souza, Errol B. De

doi:10.1016/0006-8993(92)90170-e

Cited by 22 publications

(11 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For example, clorgyline has been reported to bind to sigma sites with nanomolar affinity. However, the concentration of sigma sites in white matter is low relative to other brain regions (Heroux et al . 1992) and thus it is unlikely that sigma binding sites contribute to the observed C‐11 binding in white matter.…”

Section: Discussionmentioning

confidence: 99%

Non‐MAO A binding of clorgyline in white matter in human brain

Fowler

Logan

Ding

et al. 2001

Journal of Neurochemistry

View full text Add to dashboard Cite

show abstract

Section: Discussionmentioning

confidence: 99%

Non‐MAO A binding of clorgyline in white matter in human brain

Fowler

Logan

Ding

et al. 2001

Journal of Neurochemistry

View full text Add to dashboard Cite

show abstract

“…In vitro autoradiographic studies have revealed high densities of sigma receptors in many regions throughout the rat, mouse, guinea pig, non-human primate and human central nervous systems [104][105][106][107][108][109][110][111][112][113][114][115]. In rats, the highest densities are in the hippocampus and cortex, but they are also abundant in most other brain regions, including the limbic system, cerebellum, striatum, medulla, brain stem, substantia nigra, and spinal cord.…”

Section: Distribution Of Sigma Receptors In the Central Nervous Systemmentioning

confidence: 99%

Imaging Sigma Receptors: Applications in Drug Development

Collier¹,

Waterhouse²,

Kassiou³

2007

CPD

View full text Add to dashboard Cite

Sigma receptors have been implicated in a myriad of cellular functions, biological processes and diseases. While the precise biological functions of sigma receptors have not been elucidated, recent work has shed some light on to these enigmatic systems. Sigma receptors have recently been a target of drug development related to psychiatric and neurological disorders. Sigma ligands have also been shown to modulate endothelial cell proliferation and can control angiogenesis which makes them a promising target for oncology applications. Other areas currently being investigated include treatment of gastrointestinal, cardiovascular, endocrine and immune system disorders. Of interest is that the human sigma-1 receptor gene contains a steroid binding component, and several gonadal steroids, including progesterone, testosterone and dehydroepiandrosterone (DHEA), interact with sigma-1 receptors. Of the steroids examined thus far, progesterone binds with the highest affinity to human sigma-1 receptors, with a reported affinity (Ki) as high as 30 nM while the other steroids exhibit lower affinity. For this and other reasons, sigma-1 receptors have been proposed as a link between the central nervous system and the endocrine and reproductive systems. Taken together, the above information highlights an important yet largely unexplored but promising area of research to examine the biological function and therapeutic potential of sigma receptors. This review provides an overview of the current knowledge of these sites with a focus on specific areas where in vivo sigma receptor imaging is currently being investigated.

show abstract

“…4) . DTG pharmacology has been well characterized in both human and nonhuman species (Glennon et al, 1990;Walker et al ., 1990;Heroux et al ., 1992;Mash and Zabetian, 1992;Quirion et al, 1992;Shibuya et al, 1992;Bailey and Karbon, 1993;Izenwasser et al, 1993) . In addition to DTG, we chose to characterize the pharmacology of carbetapentane and R(-) -PPAP, two other a ligands, in the rat striatum and nucleus accumbens .…”

Section: Competition Studiesmentioning

confidence: 99%

“…This hypothesis has been substantiated by recent findings reporting that (±) -7-OH-[ 3H ] -DPAT identifies a receptors in bovine brain (Schoemaker, 1993) andbrans-7-hydroxy-2 [N-n-propyl-N-(3 F-[ 1251] iodo-2'-propenyl) ] aminotetralin (brans-7-OH-P [' 25 1 ] IPAT), a 7-OH-DPAT analogue, labels o receptors in rat brain (Kung et al ., 1993) . Moreover, cross-reactions between dopaminergic and Q binding sites might be anticipated in the striatum and nucleus accumbens given that a moderate density of Q binding sites is present in both the striatum and nucleus accumbens regions (Heroux et al, 1992;Mash and Zabetian, 1992) .…”

mentioning

confidence: 99%

Identification of D₃ and σ Receptors in the Rat Striatum and Nucleus Accumbens Using (±)‐7‐Hydroxy‐N,N‐Di‐n‐[³H]Propyl‐2‐Aminotetralin and Carbetapentane

Wallace

Booze

1995

Journal of Neurochemistry

View full text Add to dashboard Cite

Cross‐reactions between dopamine D3 and σ receptor ligands were investigated using (±)‐7‐hydroxy‐N,N‐di‐n‐[3H]propyl‐2‐aminotetralin [(±)‐7‐OH‐[3H]DPAT], a putative D3‐selective radioligand, in conjunction with the unlabeled σ ligands 1,3‐di(2‐tolyl)guanidine (DTG), carbetapentane, and R(−)‐N‐(3‐phenyl‐1‐propyl)‐1‐phenyl‐2‐aminopropane [R(−)‐PPAP]. In transfected CCL1.3 mouse fibroblasts expressing the human D3 receptor, neither DTG nor carbetapentane (0.1 µM) displaced (±)‐7‐OH‐[3H]DPAT binding. R(−)‐PPAP (0.1 µM) displaced 39.6 ± 1.0% of total (±)‐7‐OH‐[3H]DPAT binding. In striatal and nucleus accumbens homogenates, (±)‐7‐OH‐[3H]DPAT labeled a single site (15–20 fmol/mg of protein) with high (1 nM) affinity. Competition analysis with carbetapentane defined both high‐ and low‐affinity sites in striatal (35 and 65%, respectively) and nucleus accumbens (59 and 41%, respectively) tissue, yet R(−)‐PPAP identified two sites in equal proportion. Carbetapentane and R(−)‐PPAP (0.1 µM) displaced ∼20–50% of total (±)‐7‐OH‐[3H]DPAT binding in striatum, nucleus accumbens, and olfactory tubercle in autoradiographic studies, with the nucleus accumbens shell subregion exhibiting the greatest displacement. To determine directly (+)‐7‐OH‐[3H]DPAT binding to σ receptors, saturation analysis was performed in the cerebellum while masking D3 receptors with 1 µM dopamine. Under these conditions (+)‐7‐OH‐[3H]DPAT labeled σ receptors with an affinity of 24 nM. These results suggest that (a) (±)‐7‐OH‐[3H]DPAT binds D3 receptors with high affinity in rat brain and (b) a significant proportion of (±)‐7‐OH‐[3H]DPAT binding consists of σ1 sites and the percentages of these sites differ among the subregions of the striatum and nucleus accumbens.

show abstract

Autoradiographic identification and characterization of σ receptors in guinea pig brain using [3H]1(cyclopropylmethyl)-4-(2′-(4≈-fluorophenyl)-2′-oxoethyl) piperidine ([3H]DuP 734), a novel σ receptor ligand

Cited by 22 publications

References 22 publications

Non‐MAO A binding of clorgyline in white matter in human brain

Non‐MAO A binding of clorgyline in white matter in human brain

Imaging Sigma Receptors: Applications in Drug Development

Identification of D₃ and σ Receptors in the Rat Striatum and Nucleus Accumbens Using (±)‐7‐Hydroxy‐N,N‐Di‐n‐[³H]Propyl‐2‐Aminotetralin and Carbetapentane

Contact Info

Product

Resources

About

Autoradiographic identification and characterization of σ receptors in guinea pig brain using [3H]1(cyclopropylmethyl)-4-(2′-(4≈-fluorophenyl)-2′-oxoethyl) piperidine ([3H]DuP 734), a novel σ receptor ligand

Cited by 22 publications

References 22 publications

Non‐MAO A binding of clorgyline in white matter in human brain

Non‐MAO A binding of clorgyline in white matter in human brain

Imaging Sigma Receptors: Applications in Drug Development

Identification of D3 and σ Receptors in the Rat Striatum and Nucleus Accumbens Using (±)‐7‐Hydroxy‐N,N‐Di‐n‐[3H]Propyl‐2‐Aminotetralin and Carbetapentane

Contact Info

Product

Resources

About

Identification of D₃ and σ Receptors in the Rat Striatum and Nucleus Accumbens Using (±)‐7‐Hydroxy‐N,N‐Di‐n‐[³H]Propyl‐2‐Aminotetralin and Carbetapentane