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Quantifying the 5-HT1A agonist action of buspirone in man.
Psychopharmacology (Berl) 2001; 158(3):224-9P

Abstract

RATIONALE

Buspirone is used as a neuroendocrine challenge in which the increase of circulating prolactin is taken as a measure of the sensitivity of central serotonergic (5-HT(1A)) pathways. Interpretation of the test is complicated, however, by the fact that buspirone possesses D(2) antagonist and 5-HT(1A) agonist activity, both of which will result in the release of prolactin. To understand the significance of prolactin secretion in response to buspirone, it is important to measure the differential actions of the two controlling pathways.

OBJECTIVE

To characterise the dual action of buspirone in stimulating the secretion of prolactin by blocking the 5-HT(1A) action with the 5-HT1A antagonist action of pindolol.

METHODS

Healthy male subjects (n=35) received buspirone (0.5 mg x kg bw(-1) orally) with and without pre-treatment with the 5-HT(1A) receptor antagonist pindolol (40 mg over 2 days, 0.5 mg x kg bw(-1) on test day). Nine subjects underwent two additional trials in which they received a placebo with and without pre-treatment with pindolol.

RESULTS

Pindolol alone caused a small but significant reduction (18%) in the tonic release of prolactin. Buspirone alone produced a robust prolactin response which was reduced to approximately half by pindolol pre-treatment. Pindolol pre-treatment also, on average, delayed the onset and peak of the prolactin response. There was wide variation among individuals both in the absolute response to buspirone and in the proportion that could be attributed to the non-serotonergic agonist action of buspirone (22-82% IQ range).

CONCLUSIONS

Our results indicate that while serotonergic pathways play a minor role in the tonic release of prolactin, the response to a buspirone challenge alone cannot be used as a simple index of central serotonergic activity. However, if two challenges are carried out, one with buspirone and the other with buspirone plus pindolol, quantitative measures can be made of the sensitivity of both the 5-HT(1A) and the putative D(2) pathways controlling prolactin release.

Authors+Show Affiliations

School of Sport and Exercise Sciences, The University of Birmingham, Edgbaston, Birmingham B15 2TT, UK. m.w.bridge@bham.ac.ukNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

11713611

Citation

Bridge, M W., et al. "Quantifying the 5-HT1A Agonist Action of Buspirone in Man." Psychopharmacology, vol. 158, no. 3, 2001, pp. 224-9.
Bridge MW, Marvin G, Thompson CE, et al. Quantifying the 5-HT1A agonist action of buspirone in man. Psychopharmacology (Berl). 2001;158(3):224-9.
Bridge, M. W., Marvin, G., Thompson, C. E., Sharma, A., Jones, D. A., & Kendall, M. J. (2001). Quantifying the 5-HT1A agonist action of buspirone in man. Psychopharmacology, 158(3), pp. 224-9.
Bridge MW, et al. Quantifying the 5-HT1A Agonist Action of Buspirone in Man. Psychopharmacology (Berl). 2001;158(3):224-9. PubMed PMID: 11713611.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Quantifying the 5-HT1A agonist action of buspirone in man. AU - Bridge,M W, AU - Marvin,G, AU - Thompson,C E, AU - Sharma,A, AU - Jones,D A, AU - Kendall,M J, PY - 2000/09/29/received PY - 2001/07/05/accepted PY - 2001/11/20/pubmed PY - 2002/2/13/medline PY - 2001/11/20/entrez SP - 224 EP - 9 JF - Psychopharmacology JO - Psychopharmacology (Berl.) VL - 158 IS - 3 N2 - RATIONALE: Buspirone is used as a neuroendocrine challenge in which the increase of circulating prolactin is taken as a measure of the sensitivity of central serotonergic (5-HT(1A)) pathways. Interpretation of the test is complicated, however, by the fact that buspirone possesses D(2) antagonist and 5-HT(1A) agonist activity, both of which will result in the release of prolactin. To understand the significance of prolactin secretion in response to buspirone, it is important to measure the differential actions of the two controlling pathways. OBJECTIVE: To characterise the dual action of buspirone in stimulating the secretion of prolactin by blocking the 5-HT(1A) action with the 5-HT1A antagonist action of pindolol. METHODS: Healthy male subjects (n=35) received buspirone (0.5 mg x kg bw(-1) orally) with and without pre-treatment with the 5-HT(1A) receptor antagonist pindolol (40 mg over 2 days, 0.5 mg x kg bw(-1) on test day). Nine subjects underwent two additional trials in which they received a placebo with and without pre-treatment with pindolol. RESULTS: Pindolol alone caused a small but significant reduction (18%) in the tonic release of prolactin. Buspirone alone produced a robust prolactin response which was reduced to approximately half by pindolol pre-treatment. Pindolol pre-treatment also, on average, delayed the onset and peak of the prolactin response. There was wide variation among individuals both in the absolute response to buspirone and in the proportion that could be attributed to the non-serotonergic agonist action of buspirone (22-82% IQ range). CONCLUSIONS: Our results indicate that while serotonergic pathways play a minor role in the tonic release of prolactin, the response to a buspirone challenge alone cannot be used as a simple index of central serotonergic activity. However, if two challenges are carried out, one with buspirone and the other with buspirone plus pindolol, quantitative measures can be made of the sensitivity of both the 5-HT(1A) and the putative D(2) pathways controlling prolactin release. SN - 0033-3158 UR - https://www.unboundmedicine.com/medline/citation/11713611/Quantifying_the_5_HT1A_agonist_action_of_buspirone_in_man_ L2 - https://dx.doi.org/10.1007/s002130100881 DB - PRIME DP - Unbound Medicine ER -