The analgesic and respiratory depressant actions of metorphamide in mice and rabbits

Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. MET induced-analgesia was naloxone reversible and potentiated by bestatin. Naloxonazine, a relatively selective mu 1 blocker, at certain dosage (50 μg per rabbit, icv), could abolish the an...

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Published inNeuropeptides (Edinburgh) Vol. 6; no. 2; pp. 121 - 131
Main Authors Xu, ShaoFen, Lu, WenXiao, Zhou, KaiRong, He, XiaoPin, Niu, ShanFu, Xu, WeiMin, Zhang, AnZhong, Weber, E., Chang, J.K.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 01.01.1985
Elsevier
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Abstract Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. MET induced-analgesia was naloxone reversible and potentiated by bestatin. Naloxonazine, a relatively selective mu 1 blocker, at certain dosage (50 μg per rabbit, icv), could abolish the analgesia but not the respiratory inhibition produced by MET. Our result indicates that mu 1 receptors mediate the MET induced-analgesia but not its respiratory effect. Since MET is a mu- and kappa-ligand with very low delta activity, the MET induced respiratory depression may be mediated by mu 2 or kappa binding sites.
AbstractList Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. Results indicates that mu 1 receptors mediate the MET induced-analgesia but not its respiratory effect. Since MEt is a mu- and kappa-ligand with very low delta activity, the MET induced respiratory depression may be mediated by mu 2 or kappa binding sites.
Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. MET induced-analgesia was naloxone reversible and potentiated by bestatin. Naloxonazine, a relatively selective mu 1 blocker, at certain dosage (50 micrograms per rabbit, icv), could abolish the analgesia but not the respiratory inhibition produced by MET. Our result indicates that mu 1 receptors mediate the MET induced-analgesia but not its respiratory effect. Since MET is a mu- and kappa-ligand with very low delta activity, the MET induced respiratory depression may be mediated by mu 2 or kappa binding sites.
Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. MET induced-analgesia was naloxone reversible and potentiated by bestatin. Naloxonazine, a relatively selective mu 1 blocker, at certain dosage (50 μg per rabbit, icv), could abolish the analgesia but not the respiratory inhibition produced by MET. Our result indicates that mu 1 receptors mediate the MET induced-analgesia but not its respiratory effect. Since MET is a mu- and kappa-ligand with very low delta activity, the MET induced respiratory depression may be mediated by mu 2 or kappa binding sites.
Author Zhang, AnZhong
Weber, E.
Xu, ShaoFen
He, XiaoPin
Niu, ShanFu
Zhou, KaiRong
Chang, J.K.
Xu, WeiMin
Lu, WenXiao
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  organization: Peninsula Labs. Inc., San Carlos, CA, USA
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crossref_primary_10_1016_S0304_3959_99_00068_8
crossref_primary_10_1111_j_1471_4159_1987_tb00946_x
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Cites_doi 10.1016/0014-2999(80)90518-X
10.1021/jo01136a022
10.1016/0024-3205(80)90470-1
10.1016/0006-8993(77)90699-0
10.1126/science.6256856
10.1152/ajplegacy.1962.203.5.763
10.3727/036012980816952587
10.1016/0024-3205(82)90387-3
10.1038/305721a0
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Issue 2
Keywords Rodentia
Rabbit
Brain (Vertebrata)
Lagomorpha
Neuropeptide
Opioid peptide
Opiate receptor μ
Biological activity
Analgesia
Vertebrata
Mammalia
Mouse
Animal
Affinity
Respiration
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PublicationDate 1985-01-01
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PublicationTitle Neuropeptides (Edinburgh)
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Elsevier
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Snippet Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. MET induced-analgesia was naloxone reversible...
Metorphamide (MET) elicited a potent, dose-dependent analgesia and respiratory depression in mice and rabbits. Results indicates that mu 1 receptors mediate...
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StartPage 121
SubjectTerms Analgesics
Animals
Biological and medical sciences
Depression, Chemical
Enkephalin, Methionine - analogs & derivatives
Enkephalin, Methionine - antagonists & inhibitors
Enkephalin, Methionine - pharmacology
Female
Injections, Intraventricular
Male
Medical sciences
Mice
Naloxone - analogs & derivatives
Naloxone - pharmacology
Neuropharmacology
Pharmacology. Drug treatments
Rabbits
Respiration - drug effects
Sensory Thresholds
Title The analgesic and respiratory depressant actions of metorphamide in mice and rabbits
URI https://dx.doi.org/10.1016/0143-4179(85)90103-9
https://www.ncbi.nlm.nih.gov/pubmed/4000426
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