PMID- 8793901
OWN - NLM
STAT- MEDLINE
DCOM- 19961203
LR  - 20190726
IS  - 0028-3908 (Print)
IS  - 0028-3908 (Linking)
VI  - 35
IP  - 4
DP  - 1996 Apr
TI  - Evaluation of anti-nociceptive effects of neuronal nicotinic acetylcholine 
      receptor (NAChR) ligands in the rat tail-flick assay.
PG  - 393-405
AB  - In the present investigation, anti-nociceptive effects of neuronal nicotinic 
      acetylcholine receptor (NAChR) ligands, (+)- and (-)-nicotine, cytisine, 
      methylcarbamylcholine (MCC), dimethylphenylpiperazinium iodide (DMPP), and 
      (+/-)-epibatidine were evaluated in the rat tail-flick assay both after 
      subcutaneous (s.c.) and intracerebroventricular (i.c.v.) administration. The 
      pharmacology of the tail-flick response to NAChR ligands after s.c. and i.c.v. 
      routes was similar. Epibatidine was the most potent ligand examined with a longer 
      duration of action than any other agonist. (-)-Nicotine was more active than 
      (+)-nicotine indicating stereospecificity. ICV administration studies indicated 
      an apparent partial agonist activity for (+)-nicotine in the tail-flick response. 
      Tail-flick responses to NAChR agonists are independent of opioid and muscarinic 
      pathways and appear to be mediated both by central and peripheral NAChR 
      recognition sites. Central administration of MCC activates both NAChR and 
      muscarinic anti-nociceptive mechanisms. Studies employing the alpha-adrenergic 
      receptor alkylating agent, phenoxybenzamine or the noradrenergic neurotoxin, 
      N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4), suggested that the 
      NAChR-noradrenergic and NAChR-serotoninergic interactions play an important role 
      in the tail-flick response. Studies employing a selective 
      alpha-bungarotoxin-sensitive NAChR receptor antagonist, methyllycaconitine (MLA), 
      suggested a minimal role for these receptors in the tail-flick response. The 
      biochemical studies also indicated that a sub-population of NAChR receptors are 
      located pre-synaptically on noradrenergic and/or serotoninergic pathways in the 
      hippocampus.
FAU - Rao, T S
AU  - Rao TS
AD  - SIBIA Neurosciences, Inc., La Jolla, CA 92037-4641, USA.
FAU - Correa, L D
AU  - Correa LD
FAU - Reid, R T
AU  - Reid RT
FAU - Lloyd, G K
AU  - Lloyd GK
LA  - eng
PT  - Journal Article
PL  - England
TA  - Neuropharmacology
JT  - Neuropharmacology
JID - 0236217
RN  - 0 (Ligands)
RN  - 0 (Nicotinic Agonists)
RN  - 0 (Nicotinic Antagonists)
RN  - 0 (Receptors, Nicotinic)
RN  - 21019-30-7 (methyllycaconitine)
RN  - X4W3ENH1CV (Norepinephrine)
RN  - X8YN71D5WC (Aconitine)
SB  - IM
MH  - Aconitine/*analogs & derivatives/pharmacology
MH  - Animals
MH  - Chromatography, High Pressure Liquid
MH  - Electrochemistry
MH  - Evaluation Studies as Topic
MH  - Injections, Intraventricular
MH  - Injections, Subcutaneous
MH  - Ligands
MH  - Male
MH  - Neurons/*drug effects
MH  - Nicotinic Agonists/*pharmacology
MH  - Nicotinic Antagonists/*pharmacology
MH  - Norepinephrine/metabolism
MH  - Pain Measurement/*methods
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Receptors, Nicotinic/*drug effects
EDAT- 1996/04/01 00:00
MHDA- 1996/04/01 00:01
CRDT- 1996/04/01 00:00
PHST- 1996/04/01 00:00 [pubmed]
PHST- 1996/04/01 00:01 [medline]
PHST- 1996/04/01 00:00 [entrez]
AID - 0028390896000135 [pii]
AID - 10.1016/0028-3908(96)00013-5 [doi]
PST - ppublish
SO  - Neuropharmacology. 1996 Apr;35(4):393-405. doi: 10.1016/0028-3908(96)00013-5.