Mol Pharmacol. 1984 May;25(3):349-51.

Structural requirements for the binding of benzodiazepines to their peripheral-type sites.

Abstract

The DS19 Friend erythroleukemia cells possess peripheral-type benzodiazepine recognition sites that are similar to those characterized in other tissues and cells. These sites recognize only specific and well-defined ligand structures. In order for the benzodiazepines to bind to these sites, an alkyl group of 3 carbons or less is required at position 1, together with a carbonyl group at position 2. In addition, the binding affinity is enhanced by 4'-halogen or 4'-methoxy substituents, and by 7- or 2'-halogens. However, the affinity is decreased by substitutions at position 3 or 4. Central-type benzodiazepine binding in brain, on the other hand, is not affected by 1-alkyl groups and is inhibited by 4'-substitutions. Furthermore, unlike the peripheral-type site, the brain receptor is stereo-selective. These results demonstrate that the two binding sites are fundamentally different in their recognition of benzodiazepine ligands.

PMID:: 6328261; [PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Molecular Biology Databases

Supplemental Content

Save items

Related citations in PubMed

Pharmacological and physiological properties of benzodiazepine binding sites in rodent brown adipose tissue. [Comp Biochem Physiol C. 1984]
Pharmacological and physiological properties of benzodiazepine binding sites in rodent brown adipose tissue.
Hirsch JD. Comp Biochem Physiol C. 1984; 77(2):339-43.
Peripheral-type benzodiazepine receptors in the central nervous system: localization to olfactory nerves. [J Neurosci. 1984]
Peripheral-type benzodiazepine receptors in the central nervous system: localization to olfactory nerves.
Anholt RR, Murphy KM, Mack GE, Snyder SH. J Neurosci. 1984 Feb; 4(2):593-603.
Purines interact with 'central' but not 'peripheral' benzodiazepine binding sites. [Neurosci Lett. 1982]
Purines interact with 'central' but not 'peripheral' benzodiazepine binding sites.
Skerritt JH, Chen Chow S, Johnston GA, Davies LP. Neurosci Lett. 1982 Dec 23; 34(1):63-8.
Review [Is the benzodiazepine binding site a receptor?]. [Encephale. 1983]
Review [Is the benzodiazepine binding site a receptor?].
Morre M, Keane P. Encephale. 1983; 9(4 Suppl 2):125B-130B.
Review Structure-activity relationships in kynurenine, diazepam and some putative endogenous ligands of the benzodiazepine receptors. [Neurosci Biobehav Rev. 1983]
Review Structure-activity relationships in kynurenine, diazepam and some putative endogenous ligands of the benzodiazepine receptors.
Lapin IP. Neurosci Biobehav Rev. 1983 Summer; 7(2):107-18.

See reviews... See all...

Cited by 8 PubMed Central articles

Translocator protein blockade reduces prostate tumor growth. [Clin Cancer Res. 2009]
Translocator protein blockade reduces prostate tumor growth.
Fafalios A, Akhavan A, Parwani AV, Bies RR, McHugh KJ, Pflug BR. Clin Cancer Res. 2009 Oct 1; 15(19):6177-84. Epub 2009 Sep 29.
Assessment of single-dose benzodiazepines on insulin secretion, insulin sensitivity and glucose effectiveness in healthy volunteers: a double-blind, placebo-controlled, randomized cross-over trial [ISRCTN08745124]. [BMC Clin Pharmacol. 2004]
Assessment of single-dose benzodiazepines on insulin secretion, insulin sensitivity and glucose effectiveness in healthy volunteers: a double-blind, placebo-controlled, randomized cross-over trial [ISRCTN08745124].
Chevassus H, Mourand I, Molinier N, Lacarelle B, Brun JF, Petit P. BMC Clin Pharmacol. 2004 Mar 4; 4:3. Epub 2004 Mar 4.
Ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in oesophageal cancer cells: involvement of the p38MAPK signalling pathway. [Br J Cancer. 2003]
Ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in oesophageal cancer cells: involvement of the p38MAPK signalling pathway.
Sutter AP, Maaser K, Barthel B, Scherübl H. Br J Cancer. 2003 Aug 4; 89(3):564-72.

See all...

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound
PubChem chemical compound records that cite the current articles. These references are taken from those provided on submitted PubChem chemical substance records. Multiple substance records may contribute to the PubChem compound record.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance
PubChem chemical substance records that cite the current articles. These references are taken from those provided on submitted PubChem chemical substance records.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Structural requirements for the binding of benzodiazepines to their peripheral-t...
Structural requirements for the binding of benzodiazepines to their peripheral-type sites.
Mol Pharmacol. 1984 May ;25(3):349-51.

PubMed
Prolonged remission of Cushing disease after treatment with cyproheptadine.
Prolonged remission of Cushing disease after treatment with cyproheptadine.
J Pediatr. 1984 Jun ;104(6):906-8.

PubMed
Defective beta adrenergic response of cystic fibrosis sweat glands in vivo and i...
Defective beta adrenergic response of cystic fibrosis sweat glands in vivo and in vitro.
J Clin Invest. 1984 Jun ;73(6):1763-71.

PubMed
Impaired vitamin D metabolism with aging in women. Possible role in pathogenesis...
Impaired vitamin D metabolism with aging in women. Possible role in pathogenesis of senile osteoporosis.
J Clin Invest. 1984 Jun ;73(6):1668-72.

PubMed
On the plight of the rural hospital.
On the plight of the rural hospital.
J Fam Pract. 1978 Mar ;6(3):477-8.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to:

Structural requirements for the binding of benzodiazepines to their peripheral-type sites.

Abstract

Publication Types, MeSH Terms, Substances

Publication Types

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Molecular Biology Databases

Supplemental Content

Save items

Related citations in PubMed

Cited by 8 PubMed Central articles

Related information

Recent activity

Simple NCBI Directory

Getting Started

Resources

Popular

Featured

NCBI Information