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BMY 7378: Partial agonist at spinal cord 5-HT(1A) receptors.

Abstract：

:Recent data indicate that BMY 7378 demonstrates high affinity, selectivity and low intrinsic activity at hippocampal 5-HT(1A) receptors, suggesting that BMY 7378 may represent the first selective 5-HT(1A) functional antagonist. The present study examined the agonist and antagonist properties of BMY 7378 at spinal cord 5-HT(1A) receptors. In electrophysiological studies, iontophoretic administration of either the 5-HT(1A) agonist 8-OH-DPAT (43.8 +/- 5.4 nA) or BMY 7378 (46.3 +/- 5.2 nA) significantly inhibited the firing rate of wide-dynamic-range dorsal horn units indicating that BMY 7378 demonstrates significant intrinsic activity at spinal cord 5-HT(1A) receptors. Concomitant BMY 7378 and 8-OH-DPAT administration identified no BMY 7378 ejection current (20-100 nA) which antagonized the 8-OH-DPAT induced inhibition of dorsal horn unit activity. In behavioral studies in the spinal rat, 8-OH-DPAT increased the animals' sensitivity to noxious levels of mechanical stimulation (ED(50) = 269 +/- 24 nmol/kg) as did BMY 7378 (ED(50) = 295 +/- 70 nmol/kg) with no statistically significant difference in the maximal response (Y(max)) observed. Concomitant BMY 7378 and 8-OH-DPAT administration identified no BMY 7378 dose (10-1100 nmol/kg) which blocked the hyperalgesic effect of 8-OH-DPAT, rather, each drug produced similar effects which were additive. Further, the 5-HT(1A) agonist effects of BMY 7378 were blocked by the 5-HT(1A) antagonist, spiperone. Therefore, both the electrophysiologic and reflex data indicate that BMY 7378 possesses significant intrinsic activity at spinal cord 5-HT(1A) receptors, and like 8-OH-DPAT is a partial agonist at these receptors. Differences in BMY 7378 intrinsic activity at spinal cord as opposed to hippocampal 5-HT(1A) receptors are discussed in terms of regional differences in G-proteins coupled to 5-HT(1A) receptors in these two CNS regions.

journal_name

Neurochem Int

journal_title

Neurochemistry international

authors

Zemlan FP,Zieleniewski-Murphy A,Maureen Murphy R,Behbehani MM

doi

10.1016/0197-0186(90)90011-h

subject

Has Abstract

pub_date

1990-01-01 00:00:00

pages

515-22

issue

4

eissn

0197-0186

issn

1872-9754

pii

0197-0186(90)90011-H

journal_volume

16

pub_type

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