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Titolo:
CANNABINOL DERIVATIVES - BINDING TO CANNABINOID RECEPTORS AND INHIBITION OF ADENYLYLCYCLASE
Autore:
RHEE MH; VOGEL Z; BARG J; BAYEWITCH M; LEVY R; HANUS L; BREUER A; MECHOULAM R;
Indirizzi:
HEBREW UNIV JERUSALEM,FAC MED,DEPT NAT PROD,EIN KEREM CAMPUS IL-91120JERUSALEM ISRAEL HEBREW UNIV JERUSALEM,FAC MED,DEPT NAT PROD IL-91120 JERUSALEM ISRAEL WEIZMANN INST SCI,DEPT NEUROBIOL IL-76100 REHOVOT ISRAEL
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 20, volume: 40, anno: 1997,
pagine: 3228 - 3233
SICI:
0022-2623(1997)40:20<3228:CD-BTC>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
TETRAHYDROCANNABINOL; DELTA-1-TETRAHYDROCANNABINOL; IDENTIFICATION; METABOLISM; CYCLASE; ACID;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
M.H. Rhee et al., "CANNABINOL DERIVATIVES - BINDING TO CANNABINOID RECEPTORS AND INHIBITION OF ADENYLYLCYCLASE", Journal of medicinal chemistry, 40(20), 1997, pp. 3228-3233

Abstract

Several derivatives of cannabinol anti the 1,1-dimethylheptyl homolog(DMM) of cannabinol were prepared and assayed for binding to the brain and the peripheral cannabinoid receptors (CB1 and CB2), as well as for activation of CB1- and CB2-mediated inhibition of adenylylcyclase. The DMH derivatives were much more potent than the pentyl (i.e., cannabinol) derivatives. 11-Hydroxycannabinol (4a) was found to bind potently to both CB1 and CB2 (K-i values of 38.0 +/- 7.2 and 26.6 +/- 5.5 nM, respectively) and to inhibit CB1-mediated adenylylcyclase with an EC50 of 58.1 +/- 6.2 nM but to cause only 20% inhibition of CB2-mediatedadenylylcyclase at 10 mu M. It behaves as a specific, though not potent, CB2 antagonist. 11-Hydroxycannabinol-DMH (4b) is a very potent agonist for both CB1 and CB2 (K-i values of 100 +/- 50 and 200 +/- 40 pM;EC50 of adenylylcyclase inhibition 56.2 +/- 4.2 and 207.5 +/- 27.8 pM, respectively).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/09/20 alle ore 16:50:25