Abstract: Delta-opioid receptor antagonists are disclosed of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, aryl, aralkyl, trans-(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 CR, wherein R is (C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.1 -C.sub.5)alkyl or RCO; X is O, S or NY, wherein Y is H or (C.sub.1 -C.sub.5)alkyl; M is N or CH; and R.sup.4 and R.sup.5 are individually H, F, Cl, Br, NO.sub.2, NH.sub.2, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkoxy or R.sup.4 and R.sup.5 together are benzo; and the pharmaceutically acceptable salts thereof.

Abstract: Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C.sub.1 -C.sub.5) alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C.sub.2 -C.sub.5)alkenyl; Z is H or OH, R' is (C.dbd.O)-A(B)(C) wherein A is selected from the group consisting of (C.sub.1 -C.sub.5)alkyl, (C.sub.2 -C.sub.5)alkenyl and (C.sub.2 -C.sub.6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C.sub.1 -C.sub.5)alkyl group optionally substituted with CO.sub.2 H, OH or phenyl and C is CO.sub.2 H, SO.sub.3 H, amino or guanidino; and R" is selected from the group consisting of NH-A(B) (C) or is guanidino; and the pharmaceutically-acceptable salts thereof.

Abstract: Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C.sub.2 -C.sub.5)alkenyl; Z is H or OH, R' is (C.dbd.O)-A(B)(C) wherein A is selected from the group consisting of (C.sub.1 -C.sub.5)alkyl, (C.sub.2 -C.sub.5)alkenyl and (C.sub.2 -C.sub.6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C.sub.1 -C.sub.5)alkyl group optionally substituted with CO.sub.2 H, OH or phenyl and C is CO.sub.2 H, SO.sub.3 H, amino or guanidino; and R" is selected from the group consisting of NH-A(B)(C) or is guanidino; and the pharmaceutically-acceptable salts thereof.

Abstract: Substituted pyrroles of the formula: ##STR1## are disclosed wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl) alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, aryl, aralkyl, trans-(C.sub.4 -C.sub.5) alkenyl, allyl or furan-2-ylalkyl; R.sup.2 is H or OH, R.sup.3 is H, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkanoyl and R.sup.4 is H or (C.sub.1 -C.sub.5) alkyl; as well as the pharmaceutically-acceptable salts thereof. These compounds are useful as analgesics and/or as selective kappa-opioid antagonists.

Abstract: Non-addictive narcotic antitussive preparations including a normally addictive narcotic analgesic cough suppressive agent and a highly selective long-acting narcotic antagonist in a pharmaceutically acceptable liquid carrier. The narcotic antagonist is an opioid receptor site-directed alkylating agent. Preparations are disclosed having the effectiveness of codeine and other opiates for cough suppression, but devoid of addictive abuse potential.

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.