Cancer Chemother Pharmacol. 1989;24(5):307-10.

Differential interactions of traditional and novel antiemetics with dopamine D2 and 5-hydroxytryptamine3 receptors.

Source

Department of Neurology, Stanford University Medical Center, CA 94305.

Abstract

The affinities of 11 drugs for both dopamine D2 and 5-hydroxytryptamine3 (5-HT3) receptor sites were determined in brain membranes. The five "traditional" antiemetics (chlorpromazine, prochlorperazine, droperidol, fluphenazine, and domperidone) displayed high affinity (less than 20 nM) for dopamine D2 receptors in corpus striatum but were inactive at 5-HT3 receptors. In contrast, five recently developed 5-HT3 antagonists (BRL 43694, ICS 205-930, zacopride, Lilly 278584, and MDL 72222) displayed nanomolar affinity for the 5-HT3 site but were inactive (greater than 10,000 nM) at the dopamine D2 receptor. Metoclopramide was unique among these agents in that it was similarly potent at dopamine D2 (240 +/- 60 nM) and 5-HT3 (120 +/- 30 nM) receptors.

PMID:: 2527092; [PubMed - indexed for MEDLINE]

Publication Types, MeSH Terms, Substances

Publication Types

Comparative Study

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

EBSCO

Other Literature Sources

COS Scholar Universe

Supplemental Content

Save items

Related citations in PubMed

Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist. [Chem Pharm Bull (Tokyo). 2002]
Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist.
Hirokawa Y, Harada H, Yoshikawa T, Yoshida N, Kato S. Chem Pharm Bull (Tokyo). 2002 Jul; 50(7):941-59.
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity. [J Med Chem. 2003]
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
Hirokawa Y, Fujiwara I, Suzuki K, Harada H, Yoshikawa T, Yoshida N, Kato S. J Med Chem. 2003 Feb 27; 46(5):702-15.
The broad-spectrum anti-emetic activity of AS-8112, a novel dopamine D2, D3 and 5-HT3 receptors antagonist. [Br J Pharmacol. 2001]
The broad-spectrum anti-emetic activity of AS-8112, a novel dopamine D2, D3 and 5-HT3 receptors antagonist.
Yoshikawa T, Yoshida N, Oka M. Br J Pharmacol. 2001 May; 133(2):253-60.
Review Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. [Mol Psychiatry. 1998]
Review Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.
Seeman P, Tallerico T. Mol Psychiatry. 1998 Mar; 3(2):123-34.
Review The psychopharmacology of 5-HT3 receptors. [Pharmacol Ther. 1990]
Review The psychopharmacology of 5-HT3 receptors.
Costall B, Naylor RJ, Tyers MB. Pharmacol Ther. 1990; 47(2):181-202.

See reviews... See all...

Cited by 2 PubMed Central articles

Interactions of metoclopramide and ergotamine with human 5-HT(3A) receptors and human 5-HT reuptake carriers. [Br J Pharmacol. 2005]
Interactions of metoclopramide and ergotamine with human 5-HT(3A) receptors and human 5-HT reuptake carriers.
Walkembach J, Brüss M, Urban BW, Barann M. Br J Pharmacol. 2005 Oct; 146(4):543-52.
Randomised trial for the prevention of delayed emesis in patients receiving high-dose cisplatin. [Br J Cancer. 1996]
Randomised trial for the prevention of delayed emesis in patients receiving high-dose cisplatin.
Matsui K, Fukuoka M, Takada M, Kusunoki Y, Yana T, Tamura K, Yoshida T, Iida K, Hirashima T, Tsukada H, et al. Br J Cancer. 1996 Jan; 73(2):217-21.

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.
Substance
PubChem chemical substance records that cite the current articles. These references are taken from those provided on submitted PubChem chemical substance records.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Differential interactions of traditional and novel antiemetics with dopamine D2 ...
Differential interactions of traditional and novel antiemetics with dopamine D2 and 5-hydroxytryptamine3 receptors.
Cancer Chemother Pharmacol. 1989 ;24(5):307-10.

PubMed
Transformation of prostaglandin D2 to isomeric prostaglandin F2 compounds by hum...
Transformation of prostaglandin D2 to isomeric prostaglandin F2 compounds by human eosinophils: a potential mast cell-eosinophil interaction.
Adv Prostaglandin Thromboxane Leukot Res. 1989 ;19:499-502.

PubMed
Natural history and inherited disorders of a lysosomal enzyme, beta-hexosaminida...
Natural history and inherited disorders of a lysosomal enzyme, beta-hexosaminidase.
J Biol Chem. 1989 Jul 5 ;264(19):10927-30.

PubMed
Patient evaluations of low back pain care from family physicians and chiropracto...
Patient evaluations of low back pain care from family physicians and chiropractors.
West J Med. 1989 Mar ;150(3):351-5.

PubMed
Gynecologic health care of women with disabilities.
Gynecologic health care of women with disabilities.
Obstet Gynecol. 1989 Jul ;74(1):75-9.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to: