Detail of "61370-87-4"

Reference

Infusion of opiates into substantia nigra protects against maximal electroshock seizures in rats

Infusion of opiates into substantia nigra protects against maximal electroshock seizures in rats. Garant, Douglas S.; Gale, Karen (Sch. Med., Georgetown Univ., Washington, DC 20007, USA). J. Pharmacol. Exp. Ther., 234(1), 45-8 (English) 1985. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 Microinfusion of morphine [57-27-2] (sulfate 50 nmol), [d-Ala2]-Met-enkephalin [61370-87-4] (35 nmol) or dynorphin A 1-13 [72957-38-1] (1 nmol) bilaterally into the substantia nigra significantly attenuated seizures induced by maximal electroshock in rats. This action was accompanied by stereotyped behavioral hyperactivity. These anticonvulsant and behavioral effects were antagonized by systemic naloxone administration; neither effect was obsd. after intranigral microinjection of dynorphin A 1-17 amide [98035-77-9] (1 nmol). These results are consistent with a m-opiate receptor-mediated inhibition of substantia nigra efferent neurons, and with the proposal that bilateral inhibition of nigral efferents attenuates seizure propagation. However, intranigral morphine failed to alter the severity of i.v. bicuculline seizures, indicating that opiate-mediated inhibition in substantia nigra is distinct from that produced by g-aminobutyric acid.

Contractor responses of the isolated colon of the mouse to morphine and some opioid peptides

Contractor responses of the isolated colon of the mouse to morphine and some opioid peptides. Fontaine, Jeanine; Reuse, Jean (Inst. Pharm., Univ. Brussels, Brussels 1050, Belg.). Br. J. Pharmacol., 85(4), 861-7 (English) 1985. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 1 Morphine [57-27-2] (1 ′ 10-8-1 ′ 10-4 M), fentanyl [437-38-7] (1 ′ 10-9-1 ′ 10-5 M), and alfentanyl [71195-58-9] (1 ′ 10-10-1 ′ 10-3 M) as well as methionine enkephalin [58569-55-4] (1 ′ 10-1-1 ′ 10-8 M), [D-Ala2, Met-5]enkephalin [61370-87-4] (1 ′ 10-12-1 ′ 10-8 M), and dynorphin A(1 - 13) [61370-87-4] (1 ′ 10-9-1 ′ 10-6 M) caused a contractor response of the longitudinal musculature of the terminal colon of the mouse. These effects were competitively antagonized by naloxone. The pA2 values obtained for naloxone antagonism of morphine and opioid peptides and the high sensitivity of the prepn. to enkephalins suggest the presence of k-opiate receptors in this prepn. but m- and k-receptors may also be present. Opiate-induced contractions in the mouse colon were abolished by tetrodotoxin and after incubation with indomethacin. Apparently, the excitatory actions of the opiates in the mouse colon are mediated via opiate receptors located on the nerves which do not release acetylcholine, noradrenaline, or 5-hydroxytryptamine. The opiates may produce their action by removing an inhibitory neural influence (the nature of which remains to be elucidated) allowing a prostaglandin-mediated effect to predominate, thereby increasing muscle tone.