Detail of "91224-37-2"

Reference

Subpopulations of substance P (SP) receptors and separate eledoisin receptors

Subpopulations of substance P (SP) receptors and separate eledoisin receptors. Rosell, Sune; Bjoerkroth, Ulla; Folkers, Karl (Dep. Pharmacol., Karolinska Inst., Stockholm S-104 01, Swed.). Subst. P--Dublin 1983, Proc. Int. Symp., 61-2. Edited by: Skrabanek, Petr; Powell, David. Boole Press: Dublin, Ire. (English) 1983. CODEN: 51TTAK. DOCUMENT TYPE: Conference CA Section: 2 (Mammalian Hormones) Specific substance P (SP) [33507-63-0] receptor-blocking agents [D-Arg1, D-Pro2, D-Trp7,9, Leu1 SP (I) [84676-91-5] and [D-Arg1, D-Trp7,9, Leu11]SP (Spantide) [91224-37-2] were used to elucidate the possible existence of subpopulations of SP receptors. The analogs did not exhibit spasmogenic activity but blocked the SP-induced contractions of the isolated guinea pig ileum and the rat urinary bladder. The affinity consts. (pA2) for I and Spantide vs. SP were 6.3 and 6.9, resp., on the guinea pig ileum prepn. and 5.3 and 5.9, resp., on the rat urinary bladder prepn. The slopes of the regression lines of the Schild plots were close to unity. Apparently, these analogs block SP receptors in a simple competitive manner. Furthermore, the fact that the pA2 values of the 2 compds. were different from each other, strongly indicates the existence of subpopulations of SP receptors. When tested on the hamster bladder, I and Spantide did not block the contractions of eledoisin [69-25-0] and of physalemin and SP. Thus, eledoisin seems to interact with receptors which are sep. from SP receptors. The possible existence of sep. eledoisin receptors indicates that apart from SP, a tachykinin ligand of the eledoisin type may exist in mammalian tissues.

Dual capsaicin effects on ureteric motility: Low dose inhibition mediated by calcitonin gene-related peptide and high dose stimulation by tachykinins?

Dual capsaicin effects on ureteric motility: Low dose inhibition mediated by calcitonin gene-related peptide and high dose stimulation by tachykinins?. Hua, X. Y.; Lundberg, J. M. (Dep. 33507-63-0 and 86933-74-6 are also occured in this study. Pharmacol., Karolinska Inst., Stockholm, Swed.). Acta Physiol. Scand., 128(3), 453-65 (English) 1986. CODEN: APSCAX. ISSN: 0001-6772. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The effects of capsaicin [404-86-4], in relation to substance P (SP) [33507-63-0], neurokinin A (NKA) [86933-74-6], neuropeptide K (NPK) [96827-05-3], and calcitonin gene-related peptide (CGRP) [83652-28-2], which coexist in local sensory nerves, on the motility of the guinea pig ureter were studied in vivo and in vitro. Capsaicin, in a low dose (10 nmol/kg) given i.v., inhibited spontaneous, peristaltic contractions, as revealed by perfusion-pressure changes of the constantly perfused ureter in vivo. This action was independent of autonomic reflexes and prostaglandin formation. Capsaicin stimulated ureteric motility at higher doses (100 and 500 nmol/kg). The dual effects of capsaicin on the ureteric contractility were absent 2 wk after systemic capsaicin treatment, which depletes sensory neuropeptides. Both NKA and NPK initiated, as well as increased, the magnitude of the peristaltic contractions of the ureter, whereas SP only caused a minor excitatory effect. The CGRP inhibited spontaneous, as well as NKA- and NPK-induced ureteric peristaltic contractions. In vitro expts. on the ureter revealed that capsaicin (10-6M) induced phasic circular muscle contractions in 60% of the expts. Addnl., NKA, NPK, and SP consistently increased the contractile activity. The NKA tachyphylaxis inhibited the contractile response to other tachykinins and capsaicin. The SP analog Spantide [91224-37-2] inhibited the contractile responses to SP, NKA, and NPK. The CGRP also inhibited the NKA- and NPK-induced contractions of the ureter in vivo. Thus, capsaicin, which induces the release of mediators from sensory nerves within the ureter, has either stimulatory or inhibitory effects on ureteric smooth muscle, depending on the in vitro dose administered. The inhibitory response at a low capsaicin dose is similar to the effect of CGRP, whereas the contractile effects at higher doses resemble the response to tachykinins. .