Butyrophenone influences on the opiate receptor

Ian Creese; Andrew P. Feinberg; Solomon H. Snyder

doi:10.1016/0014-2999(76)90277-6

Butyrophenone influences on the opiate receptor

Ian Creese, Andrew P. Feinberg, Solomon H. Snyder

School of Medicine

Research output: Contribution to journal › Article › peer-review

65 Scopus citations

Abstract

Interaction of neuroleptic drugs with the opiate receptor was investigated by inhibition of the stereospecific binding of ³H-naloxone. Benperidol and pimozide, with IC₅₀'s of 0.3-0.5 μM, were more potent than the classical opiates meperidine and propoxyphene. A systematic structure-activity relationship was evident with the basic opiate structure of a benzene and a piperidine ring preserved in active compounds. No correlation between neuroleptic activity and binding to the opiate receptor was demonstrated.

Original language	English (US)
Pages (from-to)	231-235
Number of pages	5
Journal	European Journal of Pharmacology
Volume	36
Issue number	1
DOIs	https://doi.org/10.1016/0014-2999(76)90277-6
State	Published - Mar 1976

Keywords

Butyrophenone
Neuroleptic
Opiate receptor
Pehnothiazine
Structure-activity

ASJC Scopus subject areas

Pharmacology

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10.1016/0014-2999(76)90277-6

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title = "Butyrophenone influences on the opiate receptor",

abstract = "Interaction of neuroleptic drugs with the opiate receptor was investigated by inhibition of the stereospecific binding of 3H-naloxone. Benperidol and pimozide, with IC50's of 0.3-0.5 μM, were more potent than the classical opiates meperidine and propoxyphene. A systematic structure-activity relationship was evident with the basic opiate structure of a benzene and a piperidine ring preserved in active compounds. No correlation between neuroleptic activity and binding to the opiate receptor was demonstrated.",

keywords = "Butyrophenone, Neuroleptic, Opiate receptor, Pehnothiazine, Structure-activity",

author = "Ian Creese and Feinberg, {Andrew P.} and Snyder, {Solomon H.}",

note = "Funding Information: This work was supported by The McNeil Laboratories, Inc., USPHS grant DA-00266 and NIH Fellowship DA-05328 to I.C. and RSDA Award MH-33128 to S.H.S. We thank Adele Snowman and Michael Niehauns for excellent technical assistance.",

year = "1976",

month = mar,

doi = "10.1016/0014-2999(76)90277-6",

language = "English (US)",

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pages = "231--235",

journal = "European Journal of Pharmacology",

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TY - JOUR

T1 - Butyrophenone influences on the opiate receptor

AU - Creese, Ian

AU - Feinberg, Andrew P.

AU - Snyder, Solomon H.

N1 - Funding Information: This work was supported by The McNeil Laboratories, Inc., USPHS grant DA-00266 and NIH Fellowship DA-05328 to I.C. and RSDA Award MH-33128 to S.H.S. We thank Adele Snowman and Michael Niehauns for excellent technical assistance.

PY - 1976/3

Y1 - 1976/3

N2 - Interaction of neuroleptic drugs with the opiate receptor was investigated by inhibition of the stereospecific binding of 3H-naloxone. Benperidol and pimozide, with IC50's of 0.3-0.5 μM, were more potent than the classical opiates meperidine and propoxyphene. A systematic structure-activity relationship was evident with the basic opiate structure of a benzene and a piperidine ring preserved in active compounds. No correlation between neuroleptic activity and binding to the opiate receptor was demonstrated.

AB - Interaction of neuroleptic drugs with the opiate receptor was investigated by inhibition of the stereospecific binding of 3H-naloxone. Benperidol and pimozide, with IC50's of 0.3-0.5 μM, were more potent than the classical opiates meperidine and propoxyphene. A systematic structure-activity relationship was evident with the basic opiate structure of a benzene and a piperidine ring preserved in active compounds. No correlation between neuroleptic activity and binding to the opiate receptor was demonstrated.

KW - Butyrophenone

KW - Neuroleptic

KW - Opiate receptor

KW - Pehnothiazine

KW - Structure-activity

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DO - 10.1016/0014-2999(76)90277-6

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EP - 235

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1

ER -

Butyrophenone influences on the opiate receptor

Abstract

Keywords

ASJC Scopus subject areas

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