Selective opioid receptor alkylating agents

Details Selective opioid receptor alkylating agents Selective opioid receptor alkylating agents

1981-03-19

1982-12-07

Daus, Donald G.

Harness for working animal

546 44, 546 46, 424260, C07D48908, A61K 31485

Patent

active

043628702

ABSTRACT:
A selective opioid receptor, site-directed alkylating agent useful as a narcotic antagonist and non-addictive analgesic having the formula: ##STR1## wherein R is a Michael acceptor, a haloacetamide or isothiocyanate and R' is cyclopropylmethyl, allyl or substituted allyl. The Michael acceptors may be acrylamides or esters: ##STR2## wherein R.sup.2 is alkyl or aralkyl, and salts thereof. The preparation of the compounds is described, along with experiments involving the use of the compounds.

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Caruso, et al., Science, 204, pp. 316-318 (04/20/79).

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