PMID- 2868969 OWN - NLM STAT- MEDLINE DCOM- 19860331 LR - 20190824 IS - 0306-3623 (Print) IS - 0306-3623 (Linking) VI - 17 IP - 1 DP - 1986 TI - Pharmacology of amino acid receptors on vertebrate primary afferent nerve fibres. PG - 5-11 AB - Structure-activity of primary afferent depolarising action (PAD) mediated by gamma-aminobutyrate (GABA) analogues suggests a difference between subsynaptic receptors located at fibre terminations within the dorsal horn and axonal receptors which are distributed throughout non-synaptic regions. The interaction of the bicuculline-sensitive GABA receptor (GABA A) ionophore complex with barbiturates and benzodiazepines suggests that at least three binding sites are required to explain the independent GABA-mimetic, GABA-potentiating and picrotoxin-reversing effects of such agents. Difficulties with explanation of the depressant effects of baclofen on spinal transmission, in terms of the bicuculline-resistant GABA (GABA B) receptor hypothesis, are mentioned. Glutamate-induced PAD of low threshold afferents is mediated indirectly through release of potassium. However, such terminals possess receptors (possibly autoreceptors for L-glutamate), activated by (+)2-amino-4-phosphonobutyrate, which cause depression of transmitter release. Primary afferent C-fibres possess receptors which are selectively activated by kainate and which mediate picrotoxin-resistant PAD. Such receptors may be involved in the presynaptic conditioning of C-fibre transmitter release. The peripheral terminals of vestibular primary afferents, in amphibia, possess excitatory amino acid receptors which are probably activated by the transmitter released from hair cells. FAU - Evans, R H AU - Evans RH LA - eng PT - Journal Article PT - Review PL - England TA - Gen Pharmacol JT - General pharmacology JID - 7602417 RN - 0 (Barbiturates) RN - 0 (GABA Antagonists) RN - 0 (Glutamates) RN - 0 (Receptors, Amino Acid) RN - 0 (Receptors, Cell Surface) RN - 0 (Receptors, GABA-A) RN - 3KX376GY7L (Glutamic Acid) RN - 56-12-2 (gamma-Aminobutyric Acid) RN - H789N3FKE8 (Baclofen) RN - SIV03811UC (Kainic Acid) RN - Y37615DVKC (Bicuculline) SB - IM MH - Animals MH - Baclofen/pharmacology MH - Barbiturates/pharmacology MH - Bicuculline/pharmacology MH - Dose-Response Relationship, Drug MH - GABA Antagonists MH - Glutamates/pharmacology MH - Glutamic Acid MH - Humans MH - Kainic Acid/pharmacology MH - Neurons, Afferent/*drug effects MH - Receptors, Amino Acid MH - Receptors, Cell Surface/*drug effects MH - Receptors, GABA-A/*drug effects MH - Structure-Activity Relationship MH - gamma-Aminobutyric Acid/pharmacology RF - 84 EDAT- 1986/01/01 00:00 MHDA- 1986/01/01 00:01 CRDT- 1986/01/01 00:00 PHST- 1986/01/01 00:00 [pubmed] PHST- 1986/01/01 00:01 [medline] PHST- 1986/01/01 00:00 [entrez] AID - 0306-3623(86)90003-0 [pii] AID - 10.1016/0306-3623(86)90003-0 [doi] PST - ppublish SO - Gen Pharmacol. 1986;17(1):5-11. doi: 10.1016/0306-3623(86)90003-0.